VEGFR1 antagonists(Vascular endothelial growth factor receptor 1 antagonists), VEGFR2 antagonists(Vascular endothelial growth factor receptor 2 antagonists), VEGFR3 antagonists(Vascular endothelial growth factor receptor 3 antagonists)

Therapeutic Areas

NeoplasmsDigestive System DisordersUrogenital Diseases+ [1]

Active Indication

Advanced Endometrial CarcinomaColorectal CancerMetastatic Colorectal Carcinoma+ [20]

Inactive Indication

Adenocarcinoma of large intestineAdvanced Colorectal AdenocarcinomaAdvanced gastric carcinoma+ [7]

Originator Organization

Hutchison MediPharma Ltd.

Active Organization

Hutchison MediPharma Ltd.Wuhan Xiehe Hospital Tower

HUTCHMED (China) Ltd.

+ [8]

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

China (04 Sep 2018),

Metastatic Colorectal Carcinoma

RegulationConditional marketing approval (China), Fast Track (United States), Priority Review (China), Orphan Drug (South Korea), Breakthrough Therapy (China)

Structure/Sequence

Molecular FormulaC21H19N3O5

InChIKeyBALLNEJQLSTPIO-UHFFFAOYSA-N

CAS Registry1194506-26-7

179

Clinical Trials associated with Fruquintinib

NCT05690035

/ WithdrawnPhase 2IIT

PD-1 Antibody (Tislelizumab) Combined With VEGFR 1/2/3 Inhibitor (Fruquintinib) for ARID1A-mutated Metastatic pMMR/MSS Colorectal Cancer: an Open-label, Multi-center, Phase II Clinical Trial

This is an open-label phase II study, with the aim of investigating the efficacy and safety of Tislelizumab + Fruquintinib combination therapy in ARID1A-mutated pMMR/MSS metastatic colorectal cancer who have been treated with standard chemotherapy that includes fluoropyrimidine, oxaliplatin, and irinotecan. Patients with hypermutated CRC that carries POLE/POLD1 mutations cannot be included.

Start Date01 Jul 2025

Sponsor / Collaborator

Sun Yat-Sen University

[+2]

NCT06470178

/ Not yet recruitingNot ApplicableIIT

A Real-World Study of Neoadjuvant/Conversion Therapy for Locally Advanced or Metastatic Colorectal Cancer With Chemotherapy Combined With Anti-Angiogenic Targeted Agents

Fruquintinib is already the standard third-line treatment for metastatic colorectal cancer, but the efficacy of fruquintinib in neoadjuvant and conversion therapy for locally advanced/advanced colorectal cancer has not yet been reported. This study aims to observe the efficacy and safety of fruquintinib combined with chemotherapy in neoadjuvant or conversion therapy for colorectal cancer patients in the real world.

Start Date01 May 2025

Sponsor / Collaborator

Wuhan University

NCT06464601

/ Not yet recruitingNot ApplicableIIT

A Real-World Study of Neoadjuvant/Conversion Therapy for Locally Advanced or Metastatic Gastric Cancer With Chemotherapy Combined With Immune Checkpoint Inhibitors and Anti-Angiogenic Targeted Agents

Chemotherapy, immune checkpoint inhibitors, and anti-angiogenic targeted therapies have been explored in combination for neoadjuvant and conversion therapies. However, the efficacy of the novel anti-angiogenic agent fruquintinib in combination with immune checkpoint inhibitors and chemotherapy in the neoadjuvant and conversion treatment of locally advanced or metastatic gastric cancer has not been reported. This study aims to observe the efficacy and safety of fruquintinib combined with immune checkpoint inhibitors and chemotherapy in real-world settings.

Start Date01 Apr 2025

Sponsor / Collaborator

Wuhan University

100 Clinical Results associated with Fruquintinib

100 Translational Medicine associated with Fruquintinib

100 Patents (Medical) associated with Fruquintinib

201

Literatures (Medical) associated with Fruquintinib

31 Dec 2025·Human Vaccines & Immunotherapeutics

Durable response to third-line combination therapy in a metastatic colorectal cancer patient with BRAF V600E mutation: A case report

Article

Author: Qian, Xiaoping ; Zhang, Qun ; Li, Li

In metastatic colorectal cancer (mCRC), the BRAFV600E mutation subtype is one of the subtypes with the worst prognosis. The long-term abnormal activation of multiple signaling pathways caused by the BRAF V600E mutation is closely related to the formation of BRAF inhibitor resistance and drug-resistant tumor cell subpopulations. These factors significantly impact the survival and prognosis of CRC patients. Therefore, treating mCRC patients with the BRAFV600E mutation, particularly in later stages, is challenging. We reported a case of an mCRC patient with the BRAF V600E mutation in the primary and metastatic tumors. After the failure of second-line treatment, this patient received a combination therapy including immunotherapy (tislelizumab), radiotherapy, and targeted therapy (fruquintinib). Through comprehensive imaging evaluations and continuous monitoring of tumor markers, we were astonished to observe that the patient has achieved and maintained a complete response (CR) for over 12 months. This case supports the efficacy of combination therapy in mCRC patients with the BRAF V600E mutation.

01 Mar 2025·European Journal of Cancer

Health-related quality of life associated with fruquintinib in patients with metastatic colorectal cancer: Results from the FRESCO-2 study

Article

Author: Schelman, William R ; Tomasek, Jiri ; Yu, Ziji ; Garcia-Carbonero, Rocio ; Garcia-Alfonso, Pilar ; Price, Timothy ; Geiger, Ashley ; Elez, Elena ; Yao, James ; Dasari, Arvind ; Eng, Cathy ; Kocsis, Judit ; Kania, Marek ; Tabernero, Josep ; Yoshino, Takayuki ; Chen, Lucy ; Sartore-Bianchi, Andrea ; Chong, Geoff ; Gracian, Antonio Cubillo ; Lonardi, Sara ; Randrian, Violaine ; Sobrero, Alberto ; Satoh, Taroh ; Aquino, Jeneth ; Yang, Zhao

INTRODUCTIONMaintaining or improving health-related quality of life (HRQoL) is as important as extending survival in metastatic colorectal cancer. We report an HRQoL analysis from FRESCO-2 (NCT04322539).METHODSPatients were randomized to fruquintinib +best supportive care (BSC; n = 461) or placebo +BSC (n = 230). Instruments of EORTC QLQ-C30 and 5-level EQ-5D, and ECOG performance status (PS) were assessed. Changes from baseline scores for QLQ-C30 and EQ-5D were evaluated and minimally important difference thresholds were used to define stable, improved, or deteriorated QoL. Time to deterioration (TTD) was assessed.RESULTSWith fruquintinib versus placebo, baseline QLQ-C30 global health status (GHS) and EQ-5D visual analog scale (VAS) scores were 65.2 versus 64.6 and 67.0 versus 66.6, respectively. Least-squares mean changes from baseline fluctuated throughout treatment. At end of treatment (EOT), mean scores with fruquintinib versus placebo were 53.8 versus 52.3 (QLQ-C30 GHS) and 58.9 versus 58.5 (EQ-5D VAS). For QLQ-C30 GHS, 38.3 % versus 36.5 % of patients receiving fruquintinib versus placebo had stable or improved scores at EOT; median TTD was 2.1 versus 1.8 months (HR, 0.9; 95 % CI, 0.7-1.0). For EQ-5D VAS, 47.9 % versus 42.7 % had stable or improved scores at EOT; median TTD was 2.6 versus 1.9 months (HR, 0.8; 95 % CI, 0.6-0.9). Median TTD to ECOG PS ≥ 2 or death within 30+ /7 days after EOT was 6.6 versus 2.9 months with fruquintinib versus placebo (HR, 0.6; 95 % CI, 0.4-0.7).CONCLUSIONSFruquintinib delayed TTD of ECOG PS and did not negatively impact HRQoL versus placebo.

01 Feb 2025·Clinical Oncology

Fruquintinib Combined With PD-1 Inhibitors for the Treatment of the Patients With Microsatellite Stability Metastatic Colorectal Cancer: Real-World Data

Article

Author: Cheng, X ; Li, Q ; He, L ; Gu, Y ; Zhou, C ; Zhang, B ; Tu, S

AIMSProgrammed death-1 (PD-1) or programmed death-ligand 1 (PD-L1) inhibitors have shown limited effectiveness in patients with microsatellite stable (MSS) metastatic colorectal cancer (mCRC). Combining anti-angiogenesis inhibitors with PD-1 inhibitors has the potential to reverse the immunosuppressive tumour microenvironment, synergistically enhancing the anti-tumour immune response in MSS mCRC. The goal is to present real-world data that prove the clinical efficacy and safety of fruquintinib combined with PD-1 inhibitors in MSS mCRC.MATERIALS AND METHODSWe conducted a real-world retrospective study in patients with MSS mCRC who received treatment with fruquintinib combined with PD-1 inhibitors between May 2019 and March 2023 in our centre.RESULTSSeventy seven patients with MSS mCRC received fruquintinib combined with PD-1 inhibitors. In total, 5.2% of patients (4/77) achieved a partial response (PR), while 50.6% (39/77) had a stable disease (SD). Notably, three lesions achieving PR were all lung metastases and the overall disease control rate (DCR) reached 55.8% (43/77). Median progression-free survival (PFS) and overall survival (OS) reached 5.1 months (95% CI: 3.6-6.7) and 14.6 months (95% CI: 9.6-15.6), respectively. Multivariate Cox analysis showed that prior treatment without vascular endothelial growth factor (VEGF) inhibitors was significantly associated with PFS and OS (p < 0.05). Further analysis indicated that total- or polymorphonuclear myeloid-derived suppressor cells (PMN-MDSCs) significantly decreased after treatment (P = 0.039), especially in the PR/SD group (P = 0.003). Most adverse events included abdominal pain, rash, oedema, diarrhoea, and immunotherapy-associated hypothyroidism, yet symptoms were controllable.CONCLUSIONOur results provided additional evidence that patients with MSS mCRC could benefit from the combination of fruquintinib and PD-1 inhibitors, especially those with lung metastases or without prior treatment with VEGF inhibitors. The detection of MDSCs may be an immune indicator for predicting of the combined therapy.

139

News (Medical) associated with Fruquintinib

19 Mar 2025

·www.prnewswire.com

Innovent and HUTCHMED Jointly Announce that the FRUSICA-2 Phase 2/3 Study of Sintilimab and Fruquintinib Combination Has Met Its Primary Endpoint in Advanced Renal Cell Carcinoma in China

SAN FRANCISCO and SUZHOU, China, March 18, 2025 /PRNewswire/ -- Innovent Biologics, Inc. ("Innovent") (HKEX: 01801), a world-class biopharmaceutical company that develops, manufactures and commercializes high quality medicines for the treatment of oncology, cardiovascular and metabolic, autoimmune, ophthalmology and other major diseases, and HUTCHMED (China) Limited ("HUTCHMED") (Nasdaq/AIM:HCM; HKEX:13), today jointly announce that the FRUSICA-2 Phase 2/3 clinical trial evaluating sintilimab in combination with fruquintinib as second-line treatment for locally advanced or metastatic renal cell carcinoma (RCC) in China has met its primary endpoint of progression free survival (PFS) per RECIST 1.1 as assessed by blinded independent central review (BICR). The combination of sintilimab and fruquintinib received conditional approval from China's National Medical Products Administration (NMPA) for the treatment of patients with advanced endometrial cancer with Mismatch Repair proficient (pMMR) tumors that have failed prior systemic therapy and are not candidates for curative surgery or radiation, based on data from the FRUSICA-1 study (NCT03903705). The FRUSICA-2 study is a randomized, open-label, active-controlled study to evaluate the efficacy and safety of sintilimab in combination with fruquintinib versus axitinib or everolimus monotherapy for the second-line treatment of advanced RCC (NCT05522231). In addition to the primary endpoint PFS, the combination also demonstrated improvements in secondary endpoints, including objective response rate (ORR) and duration of response (DoR). Full results will be submitted for presentation at an upcoming scientific conference. Prof Dingwei Ye of Fudan University Shanghai Cancer Center and the co-leading Principal Investigator of the FRUSICA-2 study, said: "The rapid advancements in targeted therapies, immunotherapies, and their combination regimens have led to a significant evolution in the treatment landscape for advanced renal cell carcinoma. Targeted therapy remains an indispensable and crucial component in systemic treatment of advanced RCC in China. Optimizing the selection of targeted therapy, either as monotherapy or in combination with immunotherapy, for individual patients is a key focus of clinical interest. The results from the FRUSICA 2 study underscore the potential of the sintilimab and fruquintinib combination to address the pressing medical needs of patients with this challenging disease." Prof Zhisong He of Peking University First Hospital and the co-leading Principal Investigator of the FRUSICA-2 study, said: "The positive results from this Phase 3 study of the sintilimab and fruquintinib combination represent a significant advancement in the treatment of advanced renal cell carcinoma. We are optimistic about the clinical implications of the findings as we strive to provide more effective treatment options for patients who may not have had adequate responses to previous therapies." Dr Hui Zhou, Senior Vice President of Innovent, stated: "We are encouraged by the positive results in the FRUSICA-2 clinical trial. These outcomes not only underscore the great potential of the combination therapy of sintilimab and fruquintinib but also bring new hope to previously treated patients with advanced renal cell carcinoma. We look forward to working closely with HUTCHMED to jointly advance the registrational communication of this innovative combo therapy and make it available to patients as soon as possible." Dr Michael Shi, Head of R&D and Chief Medical Officer of HUTCHMED, stated: "The encouraging results from our study provide clear evidence for the combination of fruquintinib and sintilimab as a viable new treatment option for advanced renal cell carcinoma patients who have progressed on previous therapy. This not only reaffirms our commitment to advancing cancer therapies but also represents an important step forward in addressing unmet medical needs within this patient population. I extend my heartfelt gratitude to the patients and investigators who participated in this research; their contributions have been vital to our success. We look forward to sharing detailed findings with regulatory authorities and progressing toward NDA filings in the coming months." About Kidney Cancer and RCC It is estimated that approximately 435,000 new patients were diagnosed with kidney cancer worldwide in 2022.[i] In China, an estimated 74,000 new patients were diagnosed with kidney cancer in 2022.[ii] Approximately 90% of kidney tumors are RCC. About Sintilimab Sintilimab, marketed as TYVYT® (sintilimab injection) in China, is a PD-1 immunoglobulin G4 monoclonal antibody co-developed by Innovent and Eli Lilly and Company. Sintilimab is a type of immunoglobulin G4 monoclonal antibody, which binds to PD-1 molecules on the surface of T-cells, blocks the PD-1 / PD-Ligand 1 (PD-L1) pathway, and reactivates T-cells to kill cancer cells.[iii] In China, sintilimab has been approved and included in the updated NRDL for seven indications. The updated NRDL reimbursement scope for TYVYT® (sintilimab injection) includes: For the treatment of relapsed or refractory classic Hodgkin's lymphoma after two lines or later of systemic chemotherapy; For the first-line treatment of unresectable locally advanced or metastatic non-squamous non-small cell lung cancer lacking EGFR or ALK driver gene mutations; For the treatment of patients with EGFR-mutated locally advanced or metastatic non-squamous non-small cell lung cancer who progressed after EGFR-TKI therapy; For the first-line treatment of unresectable locally advanced or metastatic squamous non-small cell lung cancer; For the first-line treatment of unresectable or metastatic hepatocellular carcinoma with no prior systematic treatment; For the first-line treatment of unresectable locally advanced, recurrent or metastatic esophageal squamous cell carcinoma; For the first-line treatment of unresectable locally advanced, recurrent or metastatic gastric or gastroesophageal junction adenocarcinoma. Furthermore, sintilimab's eighth indication, in combination with fruquintinib for the treatment of patients with advanced endometrial cancer with pMMR tumors that have failed prior systemic therapy and are not candidates for curative surgery or radiation, was conditional approved by the NMPA in December 2024. And the NDA for sintilimab in combination with ipilimumab as neoadjuvant treatment for resectable MSI-H/dMMR colon cancer is under the NMPA review and has been granted Priority Review designation. In addition, three clinical studies of sintilimab have met their primary endpoints: Phase 2 study of sintilimab monotherapy as second-line treatment of esophageal squamous cell carcinoma; Phase 3 study of sintilimab monotherapy as second-line treatment for squamous non-small cell lung cancer with disease progression following platinum-based chemotherapy; Phase 2/3 study of sintilimab in combination with fruquintinib versus axitinib or everolimus monotherapy for the second-line treatment of advanced RCC. About Fruquintinib Fruquintinib is a selective oral inhibitor of all three vascular endothelial growth factor (VEGF) receptors (VEGFR-1, -2 and -3). VEGFR inhibitors play a pivotal role in inhibiting tumor angiogenesis. Fruquintinib was designed to have enhanced selectivity that limits off-target kinase activity, allowing for drug exposure that achieves sustained target inhibition and flexibility for potential use as part of a combination therapy.[iv] About Fruquintinib Approvals Fruquintinib is co-developed and co-marketed in China by HUTCHMED and Eli Lilly and Company under the brand name ELUNATE®. It is approved for the treatment of patients with metastatic colorectal cancer who have previously received fluoropyrimidine, oxaliplatin and irinotecan-based chemotherapy, and those who have previously received or are not suitable for receiving anti-VEGF therapy or anti-epidermal growth factor receptor (EGFR) therapy (RAS wild-type) in China. It was included in the China National Reimbursement Drug List (NRDL) in January 2020. Since its launch in China, over 100,000 patients with colorectal cancer have been treated with fruquintinib. The combination of ELUNATE® (fruquintinib) and TYVYT® (sintilimab injection) has conditional approval in China for the treatment of patients with advanced endometrial cancer with Mismatch Repair proficient (pMMR) tumors that have failed prior systemic therapy and are not candidates for curative surgery or radiation. Takeda holds the exclusive worldwide license to further develop, commercialize, and manufacture fruquintinib outside mainland China, Hong Kong and Macau, marketing it under the brand name FRUZAQLA®. Fruquintinib received approval for the treatment of previously treated metastatic colorectal cancer in the US in November 2023, in the EU in June 2024, in Switzerland and Argentina in August 2024, in Canada, Japan and the United Kingdom in September 2024, in Australia and Singapore in October 2024 and in Israel and the United Arab Emirates in December 2024. Regulatory applications are progressing in many other jurisdictions. The global regulatory submissions are based on data from two large, randomized, controlled Phase III trials in colorectal cancer, the global, multi-regional FRESCO-2 trial and the FRESCO trial conducted in China, showing consistent benefit among a total of 734 metastatic colorectal cancer patients treated with fruquintinib. Safety profiles were consistent across trials. Results from the FRESCO-2 trial were published in The Lancet in June 2023,[v] while results from the FRESCO trial were published in The Journal of the American Medical Association, JAMA.[vi] The safety and efficacy of fruquintinib for the following investigational uses have not been established and there is no guarantee that it will receive health authority approval or become commercially available in any country for the uses being investigated: About Fruquintinib for Second-line Treatment of RCC The U.S. Food and Drug Administration (FDA) has approved five immune-oncology combination therapies for the first-line treatment of advanced RCC. However, only one immune-oncology combination therapy has been approved in China for advanced RCC patients classified as having intermediate or poor risk by the International mRCC Database Consortium (IMDC). Single-agent targeted therapy continues to be one of the primary choices for first-line treatment of advanced RCC in China. Notably, advanced RCC patients who have experienced failure with single-agent targeted therapy previously still indicate an unmet medical need. Results from a proof-of-concept Phase Ib/II study of fruquintinib plus sintilimab were published in Targeted Oncology in January 2025. The combination demonstrated promising efficacy and a tolerable safety profile in this setting. At the data cutoff of October 9, 2024, all 20 enrolled previously treated patients were evaluable for efficacy, with a median follow-up duration of 45.7 months. The confirmed ORR was 60.0% and DCR was 85.0%. Median DoR was 13.9 months and median PFS was 15.9 months. Overall survival ("OS") was not reached, and the 36-month OS rate was 58.3%.[vii] About Innovent Innovent is a leading biopharmaceutical company founded in 2011 with the mission to empower patients worldwide with affordable, high-quality biopharmaceuticals. The company discovers, develops, manufactures and commercializes innovative medicines that target some of the most intractable diseases. Its pioneering therapies treat cancer, cardiovascular and metabolic, autoimmune and eye diseases. Innovent has launched 15 products in the market. It has 3 new drug applications under regulatory review, 3 assets in Phase III or pivotal clinical trials and 16 more molecules in early clinical stage. Innovent partners with over 30 global healthcare companies, including Lilly, Sanofi, Incyte, Adimab, LG Chem and MD Anderson Cancer Center. Guided by the motto, "Start with Integrity, Succeed through Action," Innovent maintains the highest standard of industry practices and works collaboratively to advance the biopharmaceutical industry so that first-rate pharmaceutical drugs can become widely accessible. For more information, visit , or follow Innovent on Facebook and LinkedIn. Statement: （1）Innovent does not recommend the use of any unapproved drug (s)/indication (s). （2）Ramucirumab (Cyramza®) and Selpercatinib (Retsevmo®) and Pirtobrutinib (Jaypirca®) were developed by Eli Lilly and Company. About HUTCHMED HUTCHMED (Nasdaq/AIM:HCM; HKEX:13) is an innovative, commercial-stage, biopharmaceutical company. It is committed to the discovery, global development and commercialization of targeted therapies and immunotherapies for the treatment of cancer and immunological diseases. Since inception, HUTCHMED has focused on bringing drug candidates from in-house discovery to patients around the world, with its first three medicines marketed in China, the first of which is also approved around the world including in the US, Europe and Japan. For more information, please visit ‑med.com or follow us on LinkedIn. Forward-Looking Statements This news release may contain certain forward-looking statements that are, by their nature, subject to significant risks and uncertainties. The words "anticipate", "believe", "estimate", "expect", "intend" and similar expressions, as they relate to Innovent, are intended to identify certain of such forward-looking statements. Innovent does not intend to update these forward-looking statements regularly. These forward-looking statements are based on the existing beliefs, assumptions, expectations, estimates, projections and understandings of the management of Innovent with respect to future events at the time these statements are made. These statements are not a guarantee of future developments and are subject to risks, uncertainties and other factors, some of which are beyond Innovent's control and are difficult to predict. Consequently, actual results may differ materially from information contained in the forward-looking statements as a result of future changes or developments in our business, Innovent's competitive environment and political, economic, legal and social conditions. SOURCE Innovent Biologics WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM? 440k+ Newsrooms & Influencers 9k+ Digital Media Outlets 270k+ Journalists Opted In GET STARTED

Phase 3Clinical ResultImmunotherapyDrug ApprovalLicense out/in

13 Mar 2025

·www.fiercebiotech.com

\'I don\'t feel we lost momentum\': Takeda’s oncology execs sharpen focus after restructuring

Takeda\'s oncology leaders are focused on building off their own \"institutional knowledge.\"\n Takeda’s revamped R&D strategy means the drugmaker’s oncology leaders are prioritizing work in tumors across thoracic, gastrointestinal (GI) and hematology, while pushing the Japanese company’s cell therapy work focus to the back burner.“We\'re not doing this in a prescriptive way that would never consider anything outside of that,” Teresa Bitetti, president of Takeda’s global oncology business unit, told Fierce Biotech. “But we are looking at areas that we\'ve defined because of the white space, in terms of the unmet need, because of where the science is moving and where our strength lies.”The oncology approach meshes with the drugmaker’s new overall strategy, P.K. Morrow, M.D., head of Takeda’s oncology therapeutic area unit, told Fierce in a joint interview.In January, Takeda\'s R&D head Andy Plump, M.D., Ph.D., explained that the pharma had narrowed its focus down from 10 or 12 modalities to just four: small molecules, biologics, antibody-drug conjugates (ADCs) and allogeneic cell therapies. Of those core priorities, Takeda’s oncology leaders are taking a deep interest in ADCs, small molecules and complex biologics, Morrow said. So, everything but cell therapy.“It\'s unlikely we\'re going to do any cell therapy deals in the near future,” she said about the fourth modality.“Anytime we\'re dealing with gene therapy or cell therapy, there\'s the potential risk for a durable negative effect,” said Morrow, who joined Takeda last year after serving as Crispr Therapeutics’ chief medical officer. “It doesn\'t happen most of the time, but there\'s always the potential, right?”To protect the patient, cell and gene therapies often require extended follow-up, Morrow explained, noting that the component is an important consideration in drug development. The shift isn’t shocking—Bitetti told Fierce that Takeda wasn’t “actively pursuing” autologous cell therapies at last year’s American Society of Clinical Oncology (ASCO) conference.The sentiment shadows a broader industry trend as cell and gene companies fight to remain relevant. Most recently, Pfizer discontinued hemophilia product Beqvez, emptying its gene therapy portfolio, while bluebird bio sold for just $29 million after having at one time carried a value of $10 billion.Back at Takeda, the team still touts GDX012, also called TAK-012-1501, an allogeneic gamma delta T cell therapy the company gained from buying GammaDelta Therapeutics in 2021. The asset is currently in phase 1/2 testing for adults with acute myeloid leukemia (AML).The team will “continue for now” to pursue early-stage work in cell therapy, Bitetti said.After a wide-ranging $900 million restructure in 2024, Takeda now touts its “most robust late-stage pipeline” in the pharma’s history, consisting of six late-stage programs across 14 studies, Plump told Fierce at the beginning of the year.Developing a more mature pipeline meant that Takeda had to raise its standards, Plump said. Lifting the bar resulted in several programs being left behind, including a midstage CD19 CAR-NK cell therapy in B-cell malignancies. The asset is still being studied in a phase 1 autoimmune disease program.Momentum amid streamlining? “We did do some streamlining, but I sort of feel like we\'ve come out of the back end with a lot of energy [and] focus,” Bitetti said. “I don\'t feel like we\'ve lost momentum with it.”The restructure included implementing a more rigorous approach when considering benefit and safety thresholds that determine what programs should progress, according to Morrow. One of those programs is rusfertide, an injectable hepcidin mimetic designed to treat a rare chronic blood cancer called polycythemia vera (PV). Last year, Takeda paid out $300 million to license the asset from Protagonist Therapeutics.Just this month, the partners reported a phase 3 win, finding that rusfertide reduced blood procedures among patients with PV.Takeda’s plans to file for approval with regulatory authorities are currently “on track,” with a submission expected toward the end of this year, according to Bitetti.If rusfertide passes muster with regulators, the hepcidin mimetic peptide could go on to generate $1 billion to $2 billion in peak sales. The candidate is one of six pipeline drugs that Takeda is hoping will collectively bring in between $10 billion and $20 billion, CEO Christophe Weber said during the company’s J.P. Morgan presentation in January.Takeda isn\'t counting out China When asked about geopolitical changes, such as the BIOSECURE Act and President Donald Trump’s “America First Investment Policy,” Bitetti said Takeda isn’t counting out science from China.“One can\'t afford to ignore the innovation that\'s available today coming out of China,” she said. “It\'s not just me-toos that are coming out of China—there\'s some really interesting science.”Bitetti also cited the country’s rapid pace and ability to get the proof of concept very quickly.While she noted that companies still need to be “judicious” given the changing dynamics, she said one should “proceed at your own risk to ignore what\'s happening in China.”Meanwhile, Morrow pointed to the Japanese drugmaker’s successful partnership with Hong Kong-based Hutchmed, in which Takeda paid $400 million upfront for commercial rights outside of China to a colorectal cancer drug called fruquintinib. The oral vascular endothelial growth factor receptors (VEGFR) 1/2/3 tyrosine kinase inhibitor received FDA approval at the end of 2023 and is now marketed as Fruzaqla. Last summer, Takeda also inked a deal worth up to $1.3 billion biobucks that provides the opportunity to license Ascentage Pharma’s olverembatinib, which is being developed for chronic myeloid leukemia (CML), along with other hematological cancers. The Chinese biotech\'s third-generation BCR-ABL tyrosine kinase inhibitor is currently approved in China for certain patients with CML.As for future deals with biotechs, the leaders are looking for validated modalities in disease areas Takeda believes it can make the greatest impact in.“That\'s what you\'ll see in particular in the deals that we\'ve done in the very recent past,” Morrow said, pointing to a December deal with Keros Therapeutics that included $200 million upfront to secure ex-China rights to a molecule that could compete with Bristol Myers Squibb’s Reblozyl in blood cancer indications.The deal covers Keros’ activin inhibitor elritercept that’s in development to treat anemia tied to blood cancers such as myelodysplastic syndromes and myelofibrosis. Keros sees elritercept as a molecule that can act on all stages of platelet and red blood cell production, leading it to identify opportunities across a broad patient population.Building on strengths Takeda’s pipeline decisions also take the company’s strengths into account, Bitetti said.“We have an enormous strength on the [hematology] side,” she explained. “We have very deep relationships that go back a very long time from the early days of Velcade.”The “institutional knowledge” regarding myeloid cancers and commercializing drugs in the area is something Takeda wants to continue to build on.This is exemplified by Takeda’s purchase of oncology biotech Millennium way back in 2008, according to Morrow.The “Millennium legacy” is vital to the oncology unit because it helped Takeda better understand how to develop therapies that could become backbones to other regimens and helped draw in key talent that has expertise in precision medicine. When asked how diversity, equity and inclusion play a role in the department’s hiring practices, Bitetti said DEI considerations continue to be important.“Our position as a company hasn’t changed on diversity, in terms of doing what we think is right for the business and ensuring that we have the right breadth of perspective, not only in our clinical trials, but also how we manage the business,” Bitetti said.

Phase 3Drug ApprovalCell TherapyAcquisitionPhase 1

06 Mar 2025

·ir.cytomx.com

CytomX Therapeutics Announces 2024 Financial Results and Provides Business Update

- Continued progress with lead program, CX-2051 (EpCAM PROBODY® Topo-1 ADC), in Phase 1a study in advanced colorectal cancer with initial Phase 1a clinical data to be presented in 1H 2025 - - CX-801 (PROBODY® Interferon-alpha 2b) Phase 1a translational data in advanced melanoma expected in 2H 2025 - - Maintained financial strength with cash runway into Q2 2026 - - Company to host conference call today at 2 p.m. PST / 5 p.m. EST - SOUTH SAN FRANCISCO, Calif. , March 06, 2025 (GLOBE NEWSWIRE) -- CytomX Therapeutics, Inc. (Nasdaq: CTMX), a leader in the field of masked, conditionally activated biologics, today announced 2024 financial results and provided a business update. “Throughout 2024 we continued to advance and prioritize our multi-modality clinical pipeline with disciplined capital allocation. Entering 2025, our top strategic priority is the clinical development of our lead program, CX-2051, in advanced colorectal cancer. CX-2051 is a masked EpCAM-targeting ADC armed with a topoisomerase-1 payload, specifically designed to address profound unmet need in CRC. EpCAM is highly expressed in more than 90 percent of colorectal cancers and we believe our PROBODY platform offers a unique strategy to unlock the tremendous potential of this previously undruggable target,” said Sean McCarthy , D.Phil ., chief executive officer and chairman of CytomX. Dr. McCarthy continued, “We are encouraged by our progress to date in the first in human evaluation of CX-2051, having successfully escalated to doses predicted to be in the biologically active range. We believe CX-2051 is behaving as designed, and we look forward to sharing preliminary clinical data and future plans for CX-2051 in the coming months. We are optimistic about the potential for CX-2051 in colorectal cancer, and also in many other solid tumor types that express EpCAM and where major unmet needs remain to be addressed.” Pipeline Program Updates: CX-2051 (EpCAM PROBODY Topo-1 ADC) CX-2051 has been prioritized as Company’s lead clinical program with an initial focus in advanced metastatic CRC. The Phase 1 study of CX-2051 was initiated in April of 2024 and is focused on advanced metastatic CRC, one of many tumor types where there is high expression of EpCAM. CX-2051 contains a next generation topoisomerase-1 payload (CAMP59) and a cleavable payload-antibody linker licensed from AbbVie (formerly Immunogen). EpCAM (Epithelial Cell Adhesion Molecule) is a highly expressed tumor antigen that has been previously undruggable with systemically administered agents due to expression on normal tissues. CX-2051 is designed to open a therapeutic window for this high potential target and deliver meaningful anti-cancer activity in solid tumors, including CRC. CRC remains an area of high unmet medical need, especially in the late-line setting, where outcomes from currently approved standard of care remain extremely poor, with objective response rates in the low-single digit percentages and approximately two to four months of progression free survival1. The CX-2051 study is currently enrolling patients with advanced CRC who have generally received three or more prior lines of systemic therapy in the metastatic setting. Enrolled patients are not being pre-selected for EpCAM expression or for disease characteristics such as KRAS mutational status or liver metastases. In Phase 1 dose escalation to date, CX-2051 has demonstrated a favorable tolerability profile and doses predicted to be therapeutically active, based on preclinical modeling, have been attained. The CX-2051 Phase 1 study is ongoing and is evaluating the seventh dose level. Initial Phase 1a data in CRC are expected to be presented in the first half of 2025. CX-801 (PROBODY Interferon-alpha 2b) Phase 1 dose escalation continues with a focused early development strategy in metastatic melanoma and with the goal of initiating combination therapy with CX-801 and KEYTRUDA® in 2025. The Phase 1 study is currently in the fourth monotherapy dose escalation cohort where the dose of CX-801 exceeds the approved dose of the unmasked peginterferon alfa-2b (SYLATRON™)2. Initial Phase 1a translational and biomarker data in advanced melanoma is expected in the second half of 2025. KEYTRUDA® is a registered trademark of Merck Sharp & Dohme LLC , a subsidiary of Merck & Co., Inc., Rahway, NJ , USA CX-904 (EGFR-CD3 PROBODY TCE) Based on CX-904 clinical observations to-date as well as CytomX pipeline priorities, CytomX and Amgen have jointly decided to not further develop CX-904. Corporate and Financial: Organization: In January 2025 , CytomX announced a reduction of organizational headcount by approximately 40 percent in order to direct capital resources primarily to CX-2051 and create additional flexibility in its cost structure. Headcount reductions primarily impact areas supporting non-partnered early research and general and administrative functions and are expected to be completed by the end of the first quarter of 2025. Financial: Cost reductions realized from the January 2025 restructuring combined with focused clinical development priorities are expected to extend cash runway into the second quarter of 2026. CytomX ended 2024 with $100.6 million of cash, cash equivalents and investments. Research collaborations: New milestone achieved in Astellas T-cell engager collaboration: In February 2025 , Astellas advanced the second program to GLP toxicology studies, triggering a $5 million milestone payment to CytomX. Multiple drug discovery programs continue across our research collaborations with a focus on T-cell engagers. CytomX has research collaborations with Bristol Myers Squibb , Amgen, Astellas, Regeneron, and Moderna. New milestone achieved in Astellas T-cell engager collaboration: In February 2025 , Astellas advanced the second program to GLP toxicology studies, triggering a $5 million milestone payment to CytomX. Multiple drug discovery programs continue across our research collaborations with a focus on T-cell engagers. CytomX has research collaborations with Bristol Myers Squibb , Amgen, Astellas, Regeneron, and Moderna. __________________________________1 Lonsurf®, Fruzaqla®, Stivarga® package inserts.2 SYLATRON Prescribing Information Full Year 2024 Financial Results: Cash, cash equivalents and investments totaled $100.6 million as of December 31, 2024 , compared to $174.5 million as of December 31, 2023 . Total revenue was $138.1 million for the year ended December 31, 2024 , compared to $101.2 million in 2023. The increase in revenue was driven primarily by a higher percentage of completion for research programs in the Bristol Myers Squibb collaboration as well as the collaborations with Moderna, Astellas, and Regeneron. In 2024, CytomX remained focused on controlling costs and efficiently progressing its pipeline programs. Total operating expense in 2024 was $113.1 million compared to $107.7 million in 2023, an increase of $5.4 million . The increase in operating expenses was primarily due to a $5.0 million milestone payment to AbbVie (formerly ImmunoGen) as a result of dosing the first patient for CX-2051 in Phase 1 based upon the ImmunoGen 2019 License Agreement. Research and development expenses increased by $5.7 million during the year ended December 31, 2024 , to $83.4 million compared to $77.7 million in 2023. The $5.0 million milestone payment to AbbVie for dosing of the first patient in the CX-2051 Phase 1 study was recorded in 2024 as a research and development expense and was the primary driver of increased research and development spend in 2024 compared to 2023. General and administrative expenses were essentially flat in 2024 compared to 2023, decreasing by $0.3 million to $29.7 million for the year ended December 31, 2024 . About CytomX TherapeuticsCytomX is a clinical-stage, oncology-focused biopharmaceutical company focused on developing novel conditionally activated, masked biologics designed to be localized to the tumor microenvironment. By pioneering a novel pipeline of localized biologics, powered by its PROBODY® therapeutic platform, CytomX’s vision is to create safer, more effective therapies for the treatment of cancer. CytomX’s robust and differentiated pipeline comprises therapeutic candidates across multiple treatment modalities including antibody-drug conjugates (“ADCs”), T-cell engagers, and immune modulators such as cytokines. CytomX’s clinical-stage pipeline includes CX-2051, CX-904 and CX-801. CX-2051 is a masked, conditionally activated ADC directed toward epithelial cell adhesion molecule (EpCAM), armed with a topoisomerase-1 inhibitor payload. CX-2051 has potential applicability across multiple EpCAM-expressing epithelial cancers, including CRC, and was discovered in collaboration with ImmunoGen, now part of AbbVie. CX-904 is a masked, conditionally activated T-cell-engaging bispecific antibody targeting the epidermal growth factor receptor (EGFR) on tumor cells and the CD3 receptor on T cells. CX-904 is partnered with Amgen in a global co-development alliance. CX-801 is a masked interferon alpha-2b PROBODY® cytokine with broad potential applicability in traditionally immuno-oncology sensitive as well as insensitive (cold) tumors. CytomX has established strategic collaborations with multiple leaders in oncology, including Amgen, Astellas, Bristol Myers Squibb , Regeneron and Moderna. For more information about CytomX and how it is working to make conditionally activated treatments the new standard-of-care in the fight against cancer, visit www.cytomx.com and follow us on LinkedIn and X (formerly Twitter). CytomX Therapeutics Forward-Looking StatementsThis press release includes forward-looking statements. Such forward-looking statements involve known and unknown risks, uncertainties and other important factors that are difficult to predict, may be beyond our control, and may cause the actual results, performance, or achievements to be materially different from any future results, performance or achievements expressed or implied in such statements, including those related to the future potential of partnerships or collaboration agreements and projected cash runway. Accordingly, you should not rely on any of these forward-looking statements, including those relating to the potential benefits, safety and efficacy or progress of CytomX’s or any of its collaborative partners’ product candidates, including CX-2051 and CX-801, the potential benefits or applications of CytomX’s PROBODY® therapeutic platform, CytomX’s or its collaborative partners’ ability to develop and advance product candidates into and successfully complete clinical trials, including the ongoing and planned clinical trials of CX-2051 and CX-801 and the timing of initial and ongoing data availability for our clinical trials, including CX-2051, CX-904 and CX-801, and other development milestones. Risks and uncertainties that contribute to the uncertain nature of the forward-looking statements include: the unproven nature of CytomX’s novel PROBODY® therapeutic technology; uncertainties around the Company’s ability to raise sufficient funds to carry out its planned research and development; CytomX’s clinical trial product candidates are in the initial stages of clinical development and its other product candidates are currently in preclinical development, and the process by which preclinical and clinical development could potentially lead to an approved product is long and subject to significant risks and uncertainties, including the possibility that the results of preclinical research and early clinical trials, including initial CX-2051 and CX-801 results, may not be predictive of future results; the possibility that CytomX’s clinical trials will not be successful; the possibility that current preclinical research may not result in additional product candidates; CytomX’s dependence on the success of CX-2051 and CX-801; CytomX’s reliance on third parties for the manufacture of the Company’s product candidates; possible regulatory developments in the United States and foreign countries; and the risk that we may incur higher costs than expected for research and development or unexpected costs and expenses or may not obtain expected savings from our announced restructuring. Additional applicable risks and uncertainties include those relating to our preclinical research and development, clinical development, and other risks identified under the heading "Risk Factors" included in CytomX’s Quarterly Report on Form 10-K filed with the SEC on March 6, 2025 . The forward-looking statements contained in this press release are based on information currently available to CytomX and speak only as of the date on which they are made. CytomX does not undertake and specifically disclaims any obligation to update any forward-looking statements, whether as a result of any new information, future events, changed circumstances or otherwise. PROBODY is a U.S. registered trademark of CytomX Therapeutics, Inc. All other trademarks are the properties of their respective owners. Company Contact: Chris Ogden SVP, Chief Financial Officercogden@cytomx.com Investor Contact:Precision AQ (formerly Stern Investor Relations) Stephanie Ascher Stephanie.Ascher@precisionaq.com Media Contact: Redhouse Communications Teri Dahlman teri@redhousecomms.com Source: CytomX Therapeutics Inc.

Phase 1Financial StatementLicense out/inADC

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KEGG	Wiki	ATC	Drug Bank
D11977	-	L01XE	DB11679

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Advanced Endometrial Carcinoma	China	Hutchison MediPharma Ltd.	01 Dec 2024
Colorectal Cancer	Japan	Takeda Pharmaceutical Co., Ltd.	24 Sep 2024
Metastatic Colorectal Carcinoma	China	Hutchison MediPharma Ltd.	04 Sep 2018

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Gastroesophageal junction adenocarcinoma	NDA/BLA	China	Hutchison MediPharma Ltd.	18 Apr 2023
Stomach Cancer	NDA/BLA	China	Hutchison MediPharma Ltd.	18 Apr 2023
Metastatic Colorectal Carcinoma	NDA/BLA	United States	HUTCHMED (China) Ltd.	19 Dec 2022

Clinical Result

Indication

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Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT05971199 (ESMO_TAT2025)	Phase 2	Unresectable Hepatocellular Carcinoma	24	Fruquintinib + Sintilimab + TACE	(pmazqcyngv) = liihoudxrm gwfnoqwqsr (zdsnljsnwx, 5.8 - 21.8) View more	Positive	03 Mar 2025
NCT04322539 (FRESCO-2, Pubmed \| Eur J Cancer)	Phase 3	Metastatic Colorectal Carcinoma	-	Fruquintinib + Best Supportive Care	zlxgeztqat(ruofeubqrg) = vgtikecugh sdofujedbu (auzzcpxrbm )	Positive	01 Mar 2025
				Placebo + Best Supportive Care	zlxgeztqat(ruofeubqrg) = hxwtxvjglo sdofujedbu (auzzcpxrbm )
NCT06158919 (FDZL-FIX, ASCO_GI2025) Manual	Phase 2	HER2 negative Gastroesophageal Junction Adenocarcinoma \| HER2 negative Gastric Cancer First line	27	Fruquintinib + sintilimab/nivolumabsintilimab/nivolumab + XELOX/SOX	(otcuobamgg) = dltjrwmnzo bknugzquwc (ybddexpjyn, 5.29 - NA) View more	Positive	23 Jan 2025
NCT06010212 (ASCO_GI2025) Manual	Phase 2	Advanced Esophageal Squamous Cell Carcinoma First line	11	Fruquintinib + camrelizumab +paclitaxel liposome + nedaplatin	(xqgmxbczzf) = nimfnguday ldzikajbti (zifeopuxgb, 42.1 - 99.6) View more	Positive	23 Jan 2025
NCT05024812 (ASCO_GI2025) Manual	Phase 1/2	stomach adenocarcinoma \| Gastroesophageal junction adenocarcinoma First line \|	30	Fruquintinib + toripalimab + oxaliplatin + S-1	(gmzcwhobip) = wqcjqonfmk ovdyqhxvbc (mkzwkzbuqh, 5.68 - NA) View more	Positive	23 Jan 2025
				Fruquintinib + toripalimab + oxaliplatin + S-1 (Pts with CPS < 5)	(htomjrslfe) = zhyvwwhkix qkvruxsfbu (hwjjnpgnko )
ChiCTR2000032640 (ASCO_GI2025)	Phase 1/2	Metastatic Colorectal Carcinoma Third line KRAS mutation \| BRAF V600E mutation	39	Fruquintinib 4mg	(ayorerhpno) = qkcoaxpcyc dxwmeqwyxm (ttoxkgeofq, 12.892 - 21.708) View more	Positive	23 Jan 2025
FRESCO, FRESCO-2, FRUTIGA (ASCO_GI2025)	Phase 2/3	Gastrointestinal Neoplasms Third line	1,872	Fruquintinib	tmkgvkfgks(asslbpdusi) = The incidence of any-grade and high-grade HFSR or PPE was higher in the fruquintinib group compared to the placebo group, 27.93% vs 3.64% and 8.5% vs 0%, respectively. In the mCRC subgroup analysis, the higher incidence of any-grade and high-grade HFSR or PPE in the fruquintinib arm was also statistically significant, 29.70% vs 2.55% and 8.45% vs 0%, respectively. lhuhpftdcq (udjlpegvnt )	Positive	23 Jan 2025
				Placebo
ChiCTR2300078241 (ASCO_GI2025)	Phase 2	Metastatic Colorectal Carcinoma Third line RAS mutations	26	Fruquintinib	(wzscvqgszp) = yuodcfwrww acggjwfgec (sxdrslkclm ) View more	Positive	23 Jan 2025
				TAS-102	(wzscvqgszp) = oxkaxdnqiq acggjwfgec (sxdrslkclm ) View more
NCT04322539 (FRESCO-2, ASCO_GI2025)	Phase 3	Colorectal Cancer	-	Fruquintinib + BSC	(zsplucgupu): HR = 0.66 (95% CI, 0.55 - 0.8) View more	Positive	23 Jan 2025
				Placebo + BSC
NCT05625737 (Phase II study of fruquintinib plus sintilimab, ASCO_GI2025)	Phase 2	Advanced Gastroesophageal Junction Adenocarcinoma Second line HER2-negative	29	Fruquintinib 4mg + Sintilimab 200mg	(pjhrxmckfv) = rotrlrlbyi amkwtcbavz (vbztryphkc, 15.6 - 55.3) View more	Positive	23 Jan 2025

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