RegulationFast Track (US), Accelerated Approval (US), Priority Review (CN), Breakthrough Therapy (CN), Conditional marketing approval (CN), Orphan Drug (US)

Structure

Molecular FormulaC36H45N7O8

InChIKeyYXYAEUMTJQGKHS-UHFFFAOYSA-N

CAS Registry2389149-74-8

Clinical Trials associated with Mobocertinib Succinate

NCT06441045 / Not yet recruitingPhase 2IIT

Double Dose of Third-generation EGFR-TKI Plus Intrathecal Pemetrexed Versus Double Dose of Third-generation EGFR-TKI in NSCLC Patients With Leptomeningeal Progression Following the Treatment of Routine Dose of Third-generation EGFR-TKI: a Phase II Randomized, Multicenter Study

We aim to compare the efficacy and safety of double Dose of Third-generation EGFR-TKI Plus Intrathecal Pemetrexed Versus double Dose of Third-generation EGFR-TKI in patients with leptomeningeal progression following the treatment of routine dose of EGFR-TKI,

Start Date01 Oct 2024

Sponsor / Collaborator

Fujian Cancer Hospital

ChiCTR2400086657 / SuspendedEarly Phase 1IIT

Randomized controlled clinical study of Traditional Chinese medicine detoxification and rash reduction granules (HQZ 60) for EGFR-TKI

Start Date10 Jul 2024

Sponsor / Collaborator-

NCT06452433 / Not yet recruitingPhase 2IIT

Gumarontinib Combined With Third-generation EGFR-TKI in Patients With Locally Advanced or Metastatic Non-small Cell Lung Cancer With MET Amplification Following EGFR-TKI Treatment Failure.

This study evaluated the efficacy and safety of gumarontinib combined with third-generation EGFR-TKI in the treatment of locally advanced or metastatic NSCLC with MET amplification after first-line EGFR-TKI failure, without limiting the type of third-generation EGFR-TKI. The study was divided into 2 cohorts: Cohort 1 included patients with MET amplification after third-generation EGFR-TKI first-line therapy resistance, and cohort 2 included patients with MET amplification after first-generation EGFR-TKI first-line therapy resistance.

Start Date01 Jun 2024

Sponsor / Collaborator

Cancer Hospital Chinese Academy of Medical Sciences

100 Clinical Results associated with Mobocertinib Succinate

100 Translational Medicine associated with Mobocertinib Succinate

100 Patents (Medical) associated with Mobocertinib Succinate

5,600

Literatures (Medical) associated with Mobocertinib Succinate

01 Jan 2025·EUROPEAN JOURNAL OF HAEMATOLOGY

Choice of Frontline Tyrosine‐Kinase Inhibitor and Early Events in Very Elderly Patients With Chronic Myeloid Leukemia in Chronic Phase: A “Campus CML” Study

Article

Author: Loglisci, G. ; Capodanno, I. ; Galimberti, S. ; Crugnola, M. ; Sancetta, R. ; Breccia, M. ; Elena, C. ; Saglio, G. ; Abruzzese, E. ; Luciano, L. ; Attolico, I. ; Scortechini, A. R. ; Cavazzini, F. ; Malato, A. ; Tiribelli, M. ; Lunghi, F. ; Vincelli, D. I. ; Luzi, D. ; Miggiano, M. C. ; Crescenzi, S. Leonetti ; Russo, S. ; Bucelli, C. ; Crisà, E. ; Bonifacio, M. ; Murgano, P. ; Carmosino, I. ; Sorà, F. ; Latagliata, R. ; Annunziata, M. ; Caocci, G. ; Fava, C. ; Di Veroli, A. ; Mullai, R. ; Rapezzi, D. ; Stagno, F. ; Iurlo, A. ; Leporace, A. P. ; Bocchia, M. ; Binotto, G. ; Maggi, A. ; Sportoletti, P. ; Specchia, G.

ABSTRACT:

Objectives:

The study aimed to evaluate the utilization of frontline TKI therapy in a large cohort of elderly CP‐CML patients.

Methods:

A retrospective analysis was conducted on 332 CP‐CML patients aged 75 years or older among 1929 diagnosed from January 2012 to December 2019 followed at 36 participating Hematology Centers involved in the “Campus CML” project.

Results:

Among the patients analyzed, 85.8% received imatinib (IM) while 14.2% received second‐generation TKIs (2G‐TKI), 59.5% dasatinib, and 40.5% nilotinib. Most patients initiated IM at standard dose (67.3%) while 32.7% at reduced dose. A similar trend was observed with 2G‐TKIs. The cumulative incidence of permanent TKI discontinuation at 12 months was 28.4%, primarily due to primary resistance (10.1%) and extra‐hematologic toxicity (9.5%), with no significant difference between IM and 2G‐TKI groups. Following the introduction of generic IM in Italy in 2018, IM usage increased significantly compared with 2G‐TKIs.

Conclusions:

IM was in our Centers the preferred frontline therapy for older CP‐CML patients, with increasing utilization after the introduction of generic formulations. However, 2G‐TKIs are still used in a substantial proportion of patients, suggesting individualized physician assessments regarding patient suitability and expectations. Further investigation is needed to assess efficacy and safety of reduced TKI doses in this patient population.

31 Dec 2024·JOURNAL OF MEDICAL ECONOMICS

Real world treatment patterns, healthcare resource use and costs in patients with advanced or metastatic non-small cell lung cancer by EGFR mutation type

Article

Author: Lyle, Derek ; Lee, Inyoung ; Tian, Dajun ; Chen, Justin ; Waters, Dexter ; Vanderpoel, Julie ; Vadagam, Pratyusha ; Near, Aimee M.

AIMS:

This study described treatment patterns, healthcare resource utilization (HRU) and costs among advanced or metastatic non-small cell lung cancer (a/mNSCLC) patients with different epidermal growth factor receptor (EGFR) mutation types.

MATERIALS AND METHODS:

This retrospective study leveraged NeoGenomics NeoNucleus linked with IQVIA PharMetrics Plus between 01 January 2016 to 30 April 2021 (study period). Patients with evidence of a/mNSCLC between 01 July 2016 to 31 March 2021 (selection window) with EGFR test results indicating exon 19 deletion (exon19del), exon 21 L858R (L858R), or exon 20 insertion (exon20i) mutations were included; date of first observed evidence of a/mNSCLC was the index date. Treatment patterns, all-cause HRU and costs during ≥1 month follow-up were reported for each cohort (exon19del, L858R, and exon20i).

RESULTS:

A total of 106 exon19del, 75 L858R, and 13 exon20i patients met the study criteria. The prevalence of hospitalization was highest in the exon20i cohort (76.9%), followed by L858R (62.7%) and exon19del (55.7%) cohorts. A higher proportion of patients had evidence of hospice/end-of-life care in the exon20i (30.8%) and L858R (29.3%) cohorts relative to the exon19del cohort (22.6%). The exon20i cohort had higher median total healthcare costs per patient per month ($27,069) relative to exon19del ($17,482) and L858R ($17,763). EGFR tyrosine kinase inhibitors (TKI) were the most frequently observed treatment type for exon19del and L858R cohorts, while chemotherapy was the most observed treatment in exon20i cohort.

LIMITATIONS:

The sample size for the study cohorts was small, thus no statistical comparisons were conducted.

CONCLUSIONS:

This is one of the first real-world studies to describe HRU and costs among a/mNSCLC patients by specific EGFR mutation type. HRU and costs varied between EGFR mutation types and were highest among exon20i cohort, potentially reflecting higher disease burden and unmet need among patients with this mutation.

31 Dec 2024·Human Vaccines & Immunotherapeutics

SPP1 expression indicates outcome of immunotherapy plus tyrosine kinase inhibition in advanced renal cell carcinoma.

Article

Author: Lin, Jinglai ; Wang, Ying ; Wang, Jiahao ; Zhu, Yanjun ; Xu, Xianglai ; Wang, Jiajun ; Guo, Jianming

Clinical guidelines have recently advised combination therapy involving immunotherapy (IO) and tyrosine kinase inhibitors (TKI) as the first-line therapy approach for advanced renal cell carcinoma (RCC). Nevertheless, there is currently no available biomarker that can effectively distinguish the progression-free survival (PFS). RNA-sequencing and immunohistochemistry were conducted on our cohort of metastatic RCC patients, namely ZS-MRCC, who received combination therapy consisting of IO and TKI. We further applied RNA-sequencing, immunohistochemistry, and flow cytometry to examine the immune cell infiltration and functionality inside the tumor microenvironment of high-risk localized RCC samples. SPP1 expression was significantly higher in non-responders to IO-TKI therapy. Elevated levels of SPP1 were associated with poor PFS in both the ZS-MRCC cohort (HR = 2.73, p = .018) and validated in the JAVELIN Renal 101 cohort (HR = 1.61, p = .004). By multivariate Cox analysis, SPP1 was identified as a significant independent prognosticator. Furthermore, there existed a negative correlation between elevated levels of SPP1 and the presence of GZMB⁺CD8⁺ T cells (Spearman's ρ= -0.48, p < .001). Conversely, SPP1 expression is associated with T cell exhaustion markers. A significant increase in the abundance of Tregs was observed in tumors with high levels of SPP1. Additionally, a machine-learning-based model was constructed to predict the benefit of IO-TKI treatment. High SPP1 is associated with therapeutic resistance and unfavorable PFS in IO-TKI therapy. SPP1 expression have also been observed to be indicative of malfunction and exhaustion in T cells. Increased SPP1 expression has the potential to serve as a potential biomarker for treatment selection of metastatic RCC.

155

News (Medical) associated with Mobocertinib Succinate

04 Dec 2024

·www.prnewswire.com

Innovent and HUTCHMED Jointly Announce NMPA Conditional Approval for TYVYT® (Sintilimab Injection) in Combination with ELUNATE® (Fruquintinib) for the Treatment of Advanced Endometrial Cancer

SAN FRANCISCO, U.S. and SUZHOU, China, Dec. 3, 2024 /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)，jointly announce that the New Drug Application (NDA) for the combination of TYVYT® (sintilimab injection) and ELUNATE® (fruquintinib) has been granted 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. This approval follows the priority review status and breakthrough therapy designation by the National Medical Products Administration (NMPA) of China and marks the eighth approved indication for TYVYT® (sintilimab injection). The conditional approval by the NMPA was supported by registration stage data from FRUSICA-1, the endometrial cancer registration cohort of a multi-center, open-label Phase 2 study investigating sintilimab in combination with fruquintinib in endometrial cancer patients who have experienced disease recurrence, disease progression or intolerable toxicity with treatment on platinum-based doublet chemotherapy. Results from FRUSICA-1 were presented at the American Society of Clinical Oncology annual meeting in June 2024.[i] The study results showed that IRC-assessed ORR and DCR was 35.6% and 88.5% respectively; the combination treatment showed rapid on-set efficacy, with a median time to tumor response (mTTR) of only 1.6 months. The median PFS and OS reached 9.5 months and 21.3 months, respectively. Adverse events are consistent with those reported for similar immunotherapy and antiangiogenic agents combination treatments. Additional details can be found at clinicaltrials.gov, using identifier NCT03903705. A Phase 3 confirmatory study of the sintilimab and fruquintinib combination in this setting has been planned (NCT06584032). "This approval of sintilimab plus fruquintinib could represent a paradigm shift in managing this challenging disease. This innovative combination not only leverages the synergistic effects of targeted therapy and immunotherapy, but also addresses a critical gap in treatments available for patients with limited responses to traditional therapies," said Prof. Xiaohua Wu, Director of the Department of Gynecologic Oncology at Fudan University Affiliated Cancer Hospital and Principal Investigator of the FRUSICA-1 study. "With the promising efficacy and manageable safety profile observed in clinical trials, we are eager to have this treatment option available to patients. It brings us closer to our goal of improving survival and enhancing quality of life for patients living with advanced endometrial cancer." Dr. Hui Zhou, Senior Vice President of Innovent, stated: "The approval of sintilimab and fruquintinib combination therapy marks a meaningful advancement in the treatment landscape for advanced endometrial cancer. Together with HUTCHMED, we aim to provide a novel treatment option that improves survival rates and quality of life for patients facing limited treatment options against this aggressive cancer. TYVYT® (sintilimab injection), as a cornerstone in immuno-therapy, continues to be evaluated in clinical trials in combination with novel modalities. We remain steadfast in our commitment to reinforcing the leadership position of TYVYT® (sintilimab injection) in immuno-therapy and driving forward treatment solutions through innovation and cooperation." "This NMPA approval of fruquintinib in combination with sintilimab represents a significant advancement for patients with advanced endometrial cancer who have long awaited more effective treatments. It underscores the potential of fruquintinib to be used with other therapeutic agents to improve patient outcomes," said Dr. Michael Shi, Head of R&D and Chief Medical Officer of HUTCHMED. "It is also a testament to our ongoing efforts to extend the clinical benefit of fruquintinib to a broader patient population. We are eager to make this innovative treatment available to advanced endometrial cancer patients as soon as we can and will continue to explore further opportunities to bring hope to more patients battling cancer." About Endometrial Cancer Endometrial cancer originates in the uterus and remains a significant global health challenge. In 2020, approximately 417,000 people worldwide were diagnosed with endometrial cancer, resulting in around 97,000 deaths.[ii] Іn China alone, an estimated 82,000 new cases and 17,000 deaths were reported that year.[iii] While early-stage cases can often be surgically resected, recurrent and/or metastatic endometrial cancer remains an area of high unmet need with poor outcomes and limited treatment options.[iv],[v],[vi] 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.[vii] 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 approved by the NMPA in December 2024. In addition, two 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. 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. Fruquintinib is approved for marketing 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, where it is co-developed and co-marketed by HUTCHMED and Eli Lilly and Company under the brand name ELUNATE®. 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. In December 2024, fruquintinib was approved by NMPA in combination with sintilimab 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. 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 11 products in the market. It has 5 new drug applications under regulatory review, 3 assets in Phase III or pivotal clinical trials and 17 more molecules in early clinical stage. Innovent partners with over 30 global healthcare companies, including Eli 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) 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 and global development and commercialization of targeted therapies and immunotherapies for the treatment of cancer and immunological diseases. It has approximately 5,000 personnel across all its companies, at the center of which is a team of about 1,800 in oncology/immunology. Since inception it has focused on bringing cancer 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 in the US, Europe and Japan. For more information, please visit: ‑med.com or follow us on LinkedIn. Innovent's 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 2Drug ApprovalPhase 3Clinical ResultImmunotherapy

27 Nov 2024

·www.prnewswire.com

Kelun-Biotech's TROP2 ADC Sacituzumab tirumotecan (sac-TMT) Approved For Marketing By NMPA Of China For 2L+ Advanced or Metastatic TNBC

CHENGDU, China, Nov. 27, 2024 /PRNewswire/ -- Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. (the "Company") announced that the Company received marketing authorization in China from National Medical Products Administration (NMPA) for the first domestically developed trophoblast cell-surface antigen 2 (TROP2)-directed antibody–drug conjugate (ADC) sacituzumab tirumotecan (sac-TMT, formerly SKB264/MK-2870) for adult patients with unresectable locally advanced or metastatic triple negative breast cancer (TNBC) who have received at least two prior systemic therapies (at least one of them for advanced or metastatic setting). This is the first domestically developed TROP2 ADC approved for marketing in China and the first domestically developed ADC fully approved for marketing in China. The approval is based on the positive results from a randomized, controlled, phase 3 OptiTROP-Breast01 study in adult patients with unresectable locally advanced or metastatic TNBC who have received at least two prior systemic therapies (at least one of them for advanced or metastatic setting). Sac-TMT demonstrated statistically significant and clinically meaningful improvement in both progression-free survival (PFS) and overall survival (OS) compared to chemotherapy. The results were presented at the special clinical science symposium for next-generation ADCs at the 2024 American Society of Clinical Oncology (ASCO) Annual Meeting in May 2024. Previously, NMPA has accepted two supplemental new drug applications (sNDA) seeking the approvals of sac-TMT monotherapy for the treatment of patients with locally advanced or metastatic EGFR-mutant non-small cell lung cancer (NSCLC) following progression on EGFR-TKI therapy only, or both EGFR-TKI and platinum-based chemotherapy, respectively. Dr. Micheal Ge, CEO of Kelun-Biotech said, "It is a great pleasure to share with you the important milestone moment of the successful approval and launch of sacituzumab tirumotecan in China, which is a significant achievement of Kelun-Biotech's years of deep-rooted source innovation. As the company's first proprietary TROP2 ADC innovative drug, the successful launch of sacituzumab tirumotecan officially opens up a new pattern for the treatment of patients with 2L+ advanced TNBC. We expect that its excellent clinical efficacy and safety results will significantly enhance the clinical benefits and improve the quality of life of patients with advanced TNBC. In the future, we will continue to explore the clinical value of sacituzumab tirumotecan in other indications, maximize the market potential of sacituzumab tirumotecan, and satisfy the clinical needs of patients nationwide." ABOUT MARKET VALUE Breast cancer is a threat to women's lives and health. Among them, triple-negative breast cancer has unique biological behavioral characteristics, and is also known as the "most toxic" breast cancer. 2022 analysis of China's malignant tumor epidemiology data shows that there are 357,000 new cases of breast cancer and 75,000 deaths in Chinese women annually [1]. In the absence of effective therapeutic targets for triple-negative breast cancer, chemotherapy is the most important systemic treatment in the clinic [2], but it often has poor efficacy and high toxicity and side effects, and the prognosis is different from other subtypes of breast cancer [3], it is vital to explore more therapeutic means to improve the clinical benefit. ABOUT sac-TMT Sac-TMT, a core product of the Company, is a novel human TROP2 ADC in which the Company has proprietary intellectual property rights, targeting advanced solid tumors such as NSCLC, breast cancer (BC), gastric cancer (GC), gynecological tumors, among others. Sac-TMT is developed with a novel linker to conjugate the payload, a belotecan-derivative topoisomerase I inhibitor with a drug-to-antibody-ratio (DAR) of 7.4. Sac-TMT specifically recognizes TROP2 on the surface of tumor cells by recombinant anti-TROP2 humanized monoclonal antibodies, which is then endocytosed by tumor cells and releases KL610023 intracellularly. KL610023, as a topoisomerase I inhibitor, induces DNA damage to tumor cells, which in turn leads to cell-cycle arrest and apoptosis. In addition, it also releases KL610023 in the tumor microenvironment. Given that KL610023 is membrane permeable, it can enable a bystander effect, or in other words kill adjacent tumor cells. In May 2022, the Company licensed the exclusive rights to MSD (the tradename of Merck & Co., Inc., Rahway, NJ, USA) to develop, use, manufacture and commercialize sac-TMT in all territories outside of Greater China (includes Mainland China, Hong Kong, Macao, and Taiwan). ABOUT KELUN-BIOTECH Kelun-Biotech（6990.HK）is a holding subsidiary of Kelun Pharmaceutical (002422.SZ), which focuses on the R&D, manufacturing, commercialization and global collaboration of innovative biological drugs and small molecule drugs. The company focuses on major disease areas such as solid tumors, autoimmune, inflammatory, and metabolic diseases, and in establishing a globalized drug development and industrialization platform to address the unmet medical needs in China and the rest of world. The Company is committed to becoming a leading global enterprise in the field of innovative drugs. At present, the Company has more than 30 ongoing key innovative drug projects, of which 1 project has been approved for marketing, 3 projects are in the NDA stage, and more than 10 projects are in the clinical stage. The company has established one of the world's leading proprietary ADC platforms, OptiDC™, and has 1 ADC project approved for marketing, 1 ADC project in NDA stage, and multiple ADC or novel ADC projects in clinical or preclinical research stage. For more information, please visit . SOURCE Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM? 440k+ Newsrooms & Influencers 9k+ Digital Media Outlets 270k+ Journalists Opted In GET STARTED

Drug ApprovalPhase 3ASCOADCClinical Result

31 Oct 2024

·www.prnewswire.com

Kelun-Biotech's TROP2-ADC SKB264 (sac-TMT) Third NDA Accepted by NMPA, locally advanced or metastatic EGFR-mutant NSCLC

CHENGDU, China, Oct. 31, 2024 /PRNewswire/ -- The new drug application (NDA) (the " Application") based on the positive results from the pivotal phase III OptiTROP-Lung04 study of sacituzumab tirumotecan (sac-TMT, formerly SKB264/MK-2870) developed by Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. (the "Company") was accepted by the Center for Drug Evaluation (CDE) of the National Medical Products Administration (NMPA) of China in adult patients with epidermal growth factor receptor (EGFR)-mutant locally advanced or metastatic non-small cell lung cancer (NSCLC) who progressed after treatment with EGFR-tyrosine kinase inhibitor (TKI) therapy. OptiTROP-Lung04 is a multi-center, randomized, registrational phase III clinical study that evaluates the efficacy and safety results of sac-TMT monotherapy versus pemetrexed plus platinum chemotherapy for the treatment of patients with EGFR-mutant locally advanced or metastatic NSCLC who progressed after treatment with EGFR- TKI therapy. At a pre-specified interim analysis, sac-TMT monotherapy demonstrated a statistically significant and clinically meaningful improvement in the primary endpoint of progression-free survival (PFS) as assessed by the blinded independent review committee (BIRC) compared with pemetrexed plus platinum chemotherapy. Sac-TMT also showed a manageable safety profile, with no unexpected safety signals identified. The Application is the third NDA for sac-TMT that has been accepted by the NMPA. On October 25, 2024, it was announced on the official website of the CDE that the Application was planned to be included in the priority review and approval process of the CDE. Previously, two NDAs for sac-TMT in patients with locally advanced or metastatic triple-negative breast cancer (TNBC) who have received at least two prior systemic therapies (at least one of them for advanced or metastatic setting) and for sac-TMT monotherapy in adult patients with locally advanced or metastatic EGFR-mutant NSCLC who experience progression following treatment with an EGFR-TKI and platinum-based chemotherapy, respectively, were accepted by the NMPA. Sac-TMT, a core product of the Company, is a novel human trophoblast cell-surface antigen 2 (TROP2) antibody-drug conjugate (ADC) in which the Company has proprietary intellectual property rights, targeting advanced solid tumors such as NSCLC, breast cancer (BC), gastric cancer (GC), gynecological tumors, among others. Sac-TMT is developed with a novel linker to conjugate the payload, a belotecan-derivative topoisomerase I inhibitor with a drug-to-antibody-ratio (DAR) of 7.4. Sac-TMT specifically recognizes TROP2 on the surface of tumor cells by recombinant anti-TROP2 humanized monoclonal antibodies, which is then endocytosed by tumor cells and releases KL610023 intracellularly. KL610023, as a topoisomerase I inhibitor, induces DNA damage to tumor cells, which in turn leads to cell-cycle arrest and apoptosis. In addition, it also releases KL610023 in the tumor microenvironment. Given that KL610023 is membrane permeable, it can enable a bystander effect, or in other words kill adjacent tumor cells. In May 2022, the Company licensed the exclusive rights to MSD (the tradename of Merck & Co., Inc., Rahway, NJ, USA) to develop, use, manufacture and commercialize sac-TMT in all territories outside of Greater China (includes Mainland China, Hong Kong, Macao, and Taiwan). Dr. Micheal Ge, CEO of Kelun-Biotech, said, "sac-TMT (sacituzumab govitecan) has received its third NDA. In response to unmet clinical needs, the company has always adhered to the spirit of hard work inherent in Kelun, focusing on original innovation and doing practical work to develop new drugs with differentiated advantages and international potential. We believe that sac-TMT will shine in the field of oncology and contribute Chinese strength to the global health cause." About Kelun-Biotech Kelun-Biotech (6990.HK) is a holding subsidiary of Kelun Pharmaceutical (002422.SZ), which focuses on the R&D, manufacturing, commercialization and global collaboration of innovative biological drugs and small molecule drugs. The company focuses on major disease areas such as solid tumors, autoimmune, inflammatory, and metabolic diseases, and in establishing a globalized drug development and industrialization platform to address the unmet medical needs in China and the rest of world. The Company is committed to becoming a leading global enterprise in the field of innovative drugs. At present, the Company has more than 30 ongoing innovative projects in major disease areas such as solid tumors, autoimmune, inflammatory, and metabolic diseases, including over 10 projects in the clinical stage and 4 projects in the NDA stage with several global trials being conducted simultaneously in multiple countries, including China, Europe, and the United States. The company has established one of the world's leading proprietary ADC platforms, OptiDC™, and has 5 ADC projects in the clinical stage (2 of which are in the NDA stage) and several projects in the preclinical stage. For more information, please visit . SOURCE Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM? 440k+ Newsrooms & Influencers 9k+ Digital Media Outlets 270k+ Journalists Opted In GET STARTED

NDAPhase 3Clinical ResultPriority ReviewADC

100 Deals associated with Mobocertinib Succinate

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KEGG	Wiki	ATC	Drug Bank
D11969	-	-	-

R&D Status

Approved

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Indication	Country/Location	Organization	Date
EGFR ex20ins mutation in non-small cell lung cancer	US	Takeda Pharmaceuticals U.S.A., Inc.	15 Sep 2021

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
metastatic non-small cell lung cancer	Phase 2	-	Takeda Pharmaceutical Co., Ltd.	30 Nov 2020
Locally Advanced Lung Non-Small Cell Carcinoma	Phase 2	US	Takeda Pharmaceutical Co., Ltd.	16 Jun 2016
Locally Advanced Lung Non-Small Cell Carcinoma	Phase 2	CN	Takeda Pharmaceutical Co., Ltd.	16 Jun 2016
Locally Advanced Lung Non-Small Cell Carcinoma	Phase 2	JP	Takeda Pharmaceutical Co., Ltd.	16 Jun 2016
Locally Advanced Lung Non-Small Cell Carcinoma	Phase 2	DE	Takeda Pharmaceutical Co., Ltd.	16 Jun 2016
Locally Advanced Lung Non-Small Cell Carcinoma	Phase 2	IT	Takeda Pharmaceutical Co., Ltd.	16 Jun 2016
Locally Advanced Lung Non-Small Cell Carcinoma	Phase 2	PR	Takeda Pharmaceutical Co., Ltd.	16 Jun 2016
Locally Advanced Lung Non-Small Cell Carcinoma	Phase 2	KR	Takeda Pharmaceutical Co., Ltd.	16 Jun 2016
Locally Advanced Lung Non-Small Cell Carcinoma	Phase 2	ES	Takeda Pharmaceutical Co., Ltd.	16 Jun 2016
Locally Advanced Lung Non-Small Cell Carcinoma	Phase 2	TW	Takeda Pharmaceutical Co., Ltd.	16 Jun 2016

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


WCLC2024	Not Applicable	Non-Small Cell Lung Cancer	-	Osimertinib	xybcxzfasn(mysmwqbxbi) = xsgboyloij ehngmflryi (ikhhgsvsgn ) View more	-	07 Sep 2024
				Furmonertinib	xybcxzfasn(mysmwqbxbi) = flwfvxrpwz ehngmflryi (ikhhgsvsgn ) View more
JPRN-jRCT2051220070 (WJOG16022M, ASCO2024)	Phase 1	Solid tumor HER2 mutations	28	Mobocertinib 80 mg	uivzebyhvp(vxcnxzqpdz) = grade ≥ 3 AE occurred in 72.7% of pts; the common events (>5%) being thrombocytopenia (50.0%), diarrhea (13.6%), and anorexia (13.6%) iccraolofl (fgraregnom )	Positive	24 May 2024
NCT03811834 (phase 1 study, Pubmed)	Phase 1	EGFR exon 20 insertion mutations	-	Mobocertinib 160 mg	rquuupsire(fgyjzqdqkd) = all adverse events were Grade 1 in severity ucnisbsdcp (wmnkgyzrko )	-	24 May 2024
				[14C]-Mobocertinib 50 µg
NCT04051827 (CTgov)	Phase 1	Advanced Lung Non-Small Cell Carcinoma	26	Midazolam (Part A: Midazolam Alone)	qaedqiiezf(sffqqimjwa) = cgcwdwievg iyieecvkuo (qbukdbsufj, rcfqlpieic - etropzjahb) View more	-	12 Apr 2024
				Midazolam+Mobocertinib (Part A: Midazolam + Mobocertinib)	qaedqiiezf(sffqqimjwa) = faywccuaob iyieecvkuo (qbukdbsufj, inneojzqxj - lhywjtlpmj) View more
NCT04056455 (CTgov)	Phase 1	Neoplasms	26	Mobocertinib (Severe Renal Impairment: Mobocertinib 80 mg)	pjnffqohpe(bfsiridjuf) = ptzkxmyeya osvzxkcrbe (yuqyibcngl, moywnfmrlk - gmcfczzpha) View more	-	08 Jan 2024
				Mobocertinib (Normal Renal Function: Mobocertinib 80 mg)	pjnffqohpe(bfsiridjuf) = fpkrgkqgag osvzxkcrbe (yuqyibcngl, vmbfhsctgt - gnrzhmdyyf) View more
NCT02716116 (ESMO_ASIA2023)	Phase 1/2	Non-Small Cell Lung Cancer EGFR ex20ins-positive	57	mobocertinib	nzfpktxtnt(iccmnszzdu) = mndryeuupd xfgjngglto (yyseudzcis ) View more	-	02 Dec 2023
ESMO_ASIA2023	Not Applicable	EGFR-mutated non-small Cell Lung Cancer EGFR exon 20 insertion mutations	105	Mobocertinib	ulvtkyleuh(zkiivkusqa) = 51 patients (48.6%) reported diarrhea (all grades) related to mobocertinib (treatment discontinuation due to diarrhea: 4 patients [7.8%]) uhyofosmck (jqirjyziss )	Positive	02 Dec 2023
NCT04129502 (EXCLAIM-2, ESMO_ASIA2023)	Phase 3	EGFR exon 20 positive Neoplasms First line EGFR ex20ins+	354	Mobocertinib 160 mg PO daily	gpkidpxfhg(uokylpretw) = rlqttcwrgd sxckdbftui (wltcwlqkkb ) View more	Negative	02 Dec 2023
				Pemetrexed 500 mg/m2 plus cisplatin 75 mg/m2/carboplatin AUC 5 IV every 3 weeks for 4 cycles followed by maintenance pemetrexed	gpkidpxfhg(uokylpretw) = rnujpybkfp sxckdbftui (wltcwlqkkb ) View more
NCT04056468 (CTgov)	Phase 1	Liver Injury	24	Mobocertinib (Moderate HI (Child-Pugh B): Mobocertinib 40 mg)	alliltxzyt(qqvxozzbyx) = zdzhbmhwwm oodzuvdakv (jgppruiqah, xxhnrbcwrq - dgmunmwujv) View more	-	03 Nov 2023
				Mobocertinib (Severe HI (Child-Pugh C): Mobocertinib 40 mg)	alliltxzyt(qqvxozzbyx) = ilunslfxyy oodzuvdakv (jgppruiqah, nigfuicexi - zntyharzuj) View more
NCT03807778 (CTgov)	Phase 1	Non-Small Cell Lung Cancer	53	Mobocertinib (Mobocertinib, Phase 1 Part: All Participants)	jjeyyzprtk(fafesuormb) = dlmtldzxds dtbpxdwztf (efizglxrco, dykefvlgpx - itiihuvcfl) View more	-	03 Oct 2023
				Mobocertinib (Mobocertinib 160 mg, Phase 2 Part)	tjznyaouki(ogjqshlcrn) = thspxuiprq psvniilguw (ulpywudkqb, bcfwjtchff - wafogxqobx) View more

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