AXL inhibitors(AXL receptor tyrosine kinase inhibitors), RET inhibitors(Tyrosine-protein kinase receptor RET inhibitors), ROS1 inhibitors(Proto-oncogene tyrosine-protein kinase ROS inhibitors)

Therapeutic Areas

NeoplasmsDigestive System DisordersEndocrinology and Metabolic Disease+ [11]

Active Indication

Thyroid CancerDifferentiated Thyroid Gland CarcinomaRenal Cell Carcinoma+ [193]

Inactive Indication

Advanced breast cancerBone Marrow NeoplasmsEGFR-mutated non-small Cell Lung Cancer+ [42]

Originator Organization

Exelixis, Inc.

Active Organization

National Cancer Institute

Exelixis, Inc.

Bristol Myers Squibb Co.

+ [14]

Inactive Organization

Jiangsu Hansoh Pharmaceutical Co., Ltd.

EMD Serono, Inc.

Drug Highest PhaseApproved

First Approval Date

US (29 Nov 2012),

Thyroid Cancer, Medullary

RegulationPriority Review (US), Breakthrough Therapy (US), Fast Track (US), Orphan Drug (US)

Structure/Sequence

Molecular FormulaC32H30FN3O10

InChIKeyHFCFMRYTXDINDK-WNQIDUERSA-N

CAS Registry1140909-48-3

273

Clinical Trials associated with Cabozantinib (s)-Malate

NCT06502171

/ Not yet recruitingPhase 1IIT

A Phase 1/1b/2 Study of Cabozantinib in Combination with Selumetinib for Plexiform Neurofibroma in Adults and Adolescents with Neurofibromatosis Type 1

Based on the clinical activity of both selumetinib and cabozantinib as monotherapies in clinical trials, the demonstrated activity of these agents in reduced doses in preclinical studies, and the non-overlapping toxicity profiles, the study will assess the tolerability and efficacy of selumetinib and cabozantinib in combination in participants with NF1 ≥16 years old with progressive and/or symptomatic PN in a phase 1/1b/2 clinical trial.
Trial Design Phase 1 This will be an open label, dose escalation phase. Dose level escalation will be determined by a rolling six design. In this design, up to 6 participants can be enrolled at a given dose level and then evaluated for dose limiting toxicity (DLT) within the DLT window. The DLT window is defined as 16 weeks in this study based on the long half-life of cabozantinib and the desire to have maximum confidence about long-term tolerability of the combination prior to proceeding to the next dose level.
Phase 1b Once the recommended phase 2 dose has been determined in phase 1, an expanded cohort of 12 participants will be enrolled in phase 1b portion of the study.
Phase 2 This will be an open label, single-arm phase using the recommended phase 2 dose.

Start Date01 Jan 2025

Sponsor / Collaborator

The University of Alabama at Birmingham

[+2]

NCT05859217

/ Not yet recruitingPhase 2IIT

A Multi-center Phase II Study of Combining Cabozantinib and Atezolizumab as the 1st Line Therapy for PD-L1 Negative Advanced/Metastatic NSCLC (Cabatezo-1)

NSCLC patients with low expression level of PD-L1, esp. those with its level less than 1%, do not derive much benefit from anti-PD-1/L1 therapy (e.g. atezoilzumab). In this study, investigators hypothesize that the combination of cabozantinib (a multi-kinase inhibitor) and atezolizumab will result in better therapeutic value.

Start Date01 Dec 2024

Sponsor / Collaborator

University of Kansas

[+2]

NCT06341712

/ RecruitingPhase 2

A Phase II, Randomized, Open-label Study to Assess the Efficacy, Safety, and Pharmacokinetics (PK) of Maintenance Cabozantinib (XL184) Plus Best Supportive Care (BSC) Versus BSC in Children, Adolescents and Young Adults (AYA) With Unresectable Residual Osteosarcoma Either at Diagnosis or at First Relapse After Standard Treatment

The participants of this study will be children, adolescents, and young adults with residual osteosarcoma, which cannot be removed completely through surgery.
Participants will have achieved a partial response or stable disease at the end of conventional chemotherapy. Osteosarcoma is cancer of the bone. The cancer cells make immature bone cells, known as osteoid.
Osteosarcoma is very rare, but it is the most common type of bone cancer in children and teens. It is most common in teens and young adults.
In this study, participants will receive either cabozantinib and best supportive care or the best supportive care alone. Best supportive care will be provided at the investigator's discretion and according to institutional guidelines.
It includes antibiotics, nutritional support, correction of metabolic disorders, optimal symptom control and pain management (including radiotherapy), etc. but does not include tumor specific therapy.
Cabozantinib will be taken by mouth (orally), as a tablet, once a day. Cabozantinib will be provided to participants who tolerate it for as long as their disease does not progress. Participants in the study receiving best supportive care alone may switch to treatment with cabozantinib and best supportive care if their disease progresses and if other eligibility criteria are met.
Participants may withdraw consent to participate at any time.
The estimated duration of the study for participants is 24 months, however a participant could remain in the study longer if demonstrating treatment benefit.

Start Date22 Nov 2024

Sponsor / Collaborator

Ipsen SA

100 Clinical Results associated with Cabozantinib (s)-Malate

100 Translational Medicine associated with Cabozantinib (s)-Malate

100 Patents (Medical) associated with Cabozantinib (s)-Malate

1,804

Literatures (Medical) associated with Cabozantinib (s)-Malate

01 Feb 2025·Clinical Genitourinary Cancer

A Prospective Non-interventional Real-World Study of cabozantinib in Pretreated Patients With Advanced Renal Cell Carcinoma Refractory to Vascular Endothelial Growth Factor-Targeted Therapy (CASSIOPE)

Article

Author: Basso, Umberto ; Bigot, Pierre ; Staehler, Michael ; Rastogi, Priti ; Verzoni, Elena ; Bedke, Jens ; Hamberg, Paul ; Gajate, Pablo ; Procopio, Giuseppe ; Qvick, Bryan ; Barthelemy, Philippe ; De Vivo, Rocco ; Dutailly, Pascale ; Eymard, Jean-Christophe ; Suarez, Cristina ; Rink, Michael ; Perrot, Valérie ; Laramas, Mathieu ; Guillot, Aline ; Lázaro-Quintela, Martín

BACKGROUND:

There is a lack of published data on real-world cabozantinib use in patients with advanced renal cell carcinoma after prior vascular endothelial growth factor (VEGF)-targeted therapy.

METHODS:

CASSIOPE was a real-world, prospective, multicenter, non-interventional postauthorization safety study of cabozantinib in adult patients with advanced renal cell carcinoma in Europe following prior VEGF-targeted treatment (NCT03419572). Endpoints included cabozantinib utilization (dose modifications due to adverse events [AEs; primary endpoint], dose, dose modifications, and treatment duration), safety, effectiveness (progression-free survival [PFS], overall survival [OS], best overall response [BOR]), and healthcare resource utilization.

FINDINGS:

Full analysis set (FAS)/safety population comprised 679 patients; 433 of these initiated cabozantinib at 60 mg/day (recommended dose) (primary safety population). Median age (FAS) was 67 (range, 29-93) years; most were male (73·0%), had clear-cell histology (85·7%), metastatic disease at cabozantinib initiation (97·8%), and prior nephrectomy (80·3%). In the primary safety population, 77·1% experienced dose modification owing to an AE. In the safety population, the median daily dose was 40·0 (range, 7·8-60·0) mg/day and the median treatment duration was 7·8 (< 0·1-15·2) months. Treatment-emergent and treatment-related AEs were experienced by 95·9% and 90·4% of patients, respectively. Median PFS (FAS) assessed by the local investigator using any method was 8·3 months, and 1-year OS rate was 74%. Approximately one-third of all patients had a BOR of partial response and 6 had a complete response.

INTERPRETATION:

Second- or later-line cabozantinib was effective and manageable in a real-world setting and had a safety profile consistent with previous studies.

01 Feb 2025·Current computer-aided drug design

Discovery of Novel Pyrimidine Based Small Molecule Inhibitors as VEGFR-2 Inhibitors: Design, Synthesis, and Anti-cancer Studies

Article

Author: Dabhade, Pratap S. ; Mokale, Santosh N. ; Dhawale, Sachin A.

Background::

Receptor tyrosine kinases (RTKs) are potent oncoproteins in cancer that, when mutated or overexpressed, can cause uncontrolled growth of cells, angiogenesis, and metastasis, making them significant targets for cancer treatment. Vascular endothelial growth factor receptor 2 (VEGFR2), is a tyrosine kinase receptor that is produced in endothelial cells and is the most crucial regulator of angiogenic factors involved in tumor angiogenesis. So, a series of new substituted N-(4-((2-aminopyrimidin-5-yl)oxy)phenyl)-N-phenyl cyclopropane1,1-dicarboxamide derivatives as VEGFR-2 inhibitors have been designed and synthesized.

Methods::

Utilizing H-NMR, C13-NMR, and mass spectroscopy, the proposed derivatives were produced and assessed. HT-29 and COLO-205 cell lines were used for the cytotoxicity tests. The effective compound was investigated further for the Vegfr-2 kinase inhibition assay, cell cycle arrest, and apoptosis. A molecular docking examination was also carried out with the Maestro-12.5v of Schrodinger.

Results::

In comparison to the reference drug Cabozantinib (IC50 = 9.10 and 10.66 μM), compound SP2 revealed promising cytotoxic activity (IC50 = 4.07 and 4.98 μM) against HT-29 and COLO-205, respectively. The synthesized compound SP2 showed VEGFR-2 kinase inhibition activity with (IC50 = 6.82 μM) against the reference drug, Cabozantinib (IC50 = 0.045 μM). Moreover, compound SP2 strongly induced apoptosis by arresting the cell cycle in the G1 phase. The new compounds' potent VEGFR-2 inhibitory effect was noted with key amino acids Asp1044, and Glu883, and the hydrophobic interaction was also observed in the pocket of the VEGFR-2 active site by using a docking study.

Conclusion::

The results demonstrate that at the cellular and enzyme levels, the synthetic compounds SP2 are similarly effective as cabozantinib. The cell cycle and apoptosis data demonstrate the effectiveness of the suggested compounds. Based on the findings of docking studies, cytotoxic effects, in vitro VEGFR-2 inhibition, apoptosis, and cell cycle arrest, this research has given us identical or more effective VEGFR-2 inhibitors.

01 Feb 2025·CANCER TREATMENT REVIEWS

Dynamics of resistance to immunotherapy and TKI in patients with advanced renal cell carcinoma

Review

Author: Mollica, Veronica ; Santoni, Matteo ; Massari, Francesco ; Rizzo, Alessandro

Immune-based combinations are the cornerstone of the first-line treatment of metastatic renal cell carcinoma patients, leading to outstanding outcomes. Nevertheless, primary resistance and disease progression is a critical clinical challenge. To properly address this issue, it is pivotal to understand the mechanisms of resistance to immunotherapy and tyrosine kinase inhibitors, that tumor eventually develop under treatment. In this review of the literature, we aim at exploring resistance mechanisms arising in patients treated with first-line immune-based combinations in order to understand the biological pattern that should be investigated to overcome them. In more detail, mechanisms of resistance to nivolumab and pembrolizumab are divided into intrinsic to cancer cells and extrinsic (stromal or immune cells). Regarding axitinib, the increased expression of Nuclear protein 1 (NUPR1) or decreased levels of insulin receptor (INSR) characterize resistant cells. The secretion of non-VEGF pro-angiogenic factors, such as PDGF-BB, IL-1β, MMP-9, Gro-α, IL-8, IL-6, and CCL-2, can lead to resistance to cabozantinib. The reactivation of pathways previously targeted by lenvatinib or the activation of alternative pathways, such as EGFR-PAK2-ERK pathway, underlie the development of resistance to lenvatinib. Exploring resistance mechanism that arise during first-line therapy can lead to the development of treatment strategy able to overcome them in order to improve duration of response and patients outcomes.

353

News (Medical) associated with Cabozantinib (s)-Malate

09 Jan 2025

·www.businesswire.com

Exelixis Provides Update on Oncologic Drugs Advisory Committee Meeting for Cabozantinib (CABOMETYX®) for the Treatment of Patients with Previously Treated Advanced Neuroendocrine Tumors

ALAMEDA, Calif.--( BUSINESS WIRE )-- Exelixis, Inc. (Nasdaq: EXEL) today announced it has been notified by the U.S. Food and Drug Administration (FDA) that the supplemental New Drug Application (sNDA) for cabozantinib (CABOMETYX ® ) for the treatment of adults with previously treated advanced pancreatic neuroendocrine tumors (pNET) and advanced extra-pancreatic (epNET) will no longer be the subject of discussion at an Oncologic Drugs Advisory Committee meeting. The sNDA remains under consideration by FDA with a Prescription Drug User Fee Act action date of April 3, 2025. About Exelixis Exelixis is a globally ambitious oncology company innovating next-generation medicines and regimens at the forefront of cancer care. Powered by drug discovery and development excellence, we are rapidly evolving our product portfolio to target an expanding range of tumor types and indications with our clinically differentiated pipeline of small molecules, antibody-drug conjugates and other biotherapeutics. This comprehensive approach harnesses decades of robust investment in our science and partnerships to advance our investigational programs and extend the impact of our flagship commercial product, CABOMETYX ® (cabozantinib). Exelixis is driven by a bold scientific pursuit to create transformational treatments that give more patients hope for the future. For information about the company and its mission to help cancer patients recover stronger and live longer, visit www.exelixis.com , follow @ExelixisInc on X (Twitter), like Exelixis, Inc. on Facebook and follow Exelixis on LinkedIn. Exelixis Forward-Looking Statements This press release contains forward-looking statements, including, without limitation, statements related to: the FDA’s plans to discuss the sNDA for cabozantinib for the treatment of adults with previously treated advanced pNET and advanced epNET at an ODAC meeting; the therapeutic potential of cabozantinib as a treatment for patients with previously treated advanced pNET and advanced epNET; the regulatory review process with respect to Exelixis’ sNDA for cabozantinib in previously treated advanced pNET and advanced epNET, including the Prescription Drug User Fee Act target action date assigned by the FDA; and Exelixis’ scientific pursuit to create transformational treatments that give patients more hope for the future. Any statements that refer to expectations, projections or other characterizations of future events or circumstances are forward-looking statements and are based upon Exelixis’ current plans, assumptions, beliefs, expectations, estimates and projections. Forward-looking statements involve risks and uncertainties. Actual results and the timing of events could differ materially from those anticipated in the forward-looking statements as a result of these risks and uncertainties, which include, without limitation: complexities and the unpredictability of the regulatory review and approval processes in the U.S. and elsewhere, including the risk that the FDA may not approve cabozantinib as a treatment for pNET or epNET in a timely fashion, if at all; unexpected concerns that may arise as a result of the occurrence of adverse safety events or additional data analyses of clinical trials evaluating cabozantinib; Exelixis’ ability to protect its intellectual property rights; market competition, including the potential for competitors to obtain approval for generic versions of CABOMETYX; changes in economic and business conditions; and other factors affecting the ability of Exelixis to obtain regulatory approval for cabozantinib in new indications detailed from time to time under the caption “Risk Factors” in Exelixis’ most recent Annual Report on Form 10-K and subsequent Quarterly Reports on Form 10-Q, and in Exelixis’ future filings with the Securities and Exchange Commission. All forward-looking statements in this press release are based on information available to Exelixis as of the date of this press release, and Exelixis undertakes no obligation to update or revise any forward-looking statements contained herein, except as required by law. Exelixis, the Exelixis logo and CABOMETYX are registered U.S. trademarks of Exelixis.

NDAADCAccelerated Approval

08 Jan 2025

·www.prnewswire.com

Clarivate Identifies Eleven Potential Blockbuster and Transformative Drugs in Annual Drugs to Watch Report

Anticipated advancements in obesity, oncology, gene therapy and other areas poised to revolutionize patient care LONDON, Jan. 8, 2025 /PRNewswire/ -- Clarivate Plc (NYSE:CLVT) a leading global provider of transformative intelligence, today announced the release of the twelfth annual Drugs to Watch™ report, a trusted guide to the therapies poised to redefine the future of healthcare. This year, the highly anticipated resource highlights 11 drugs projected to achieve blockbuster status or revolutionize treatment paradigms within five years. Since its inception, Drugs to Watch has identified over 98 transformative therapies, cementing its role as an essential resource for navigating the ever-evolving pharmaceutical landscape. This year's report, powered by insights from the Clarivate Cortellis intelligence suite of products, highlights 11 therapies that have recently launched or are set to debut in 2025. These innovations, addressing critical challenges in areas such as obesity, oncology, and gene therapy, are forecast to achieve blockbuster sales by 2030 or dramatically improve patient outcomes on a global scale. The report also explores pivotal trends shaping the industry, including the surging demand for obesity treatments, the transformative potential of gene editing, and the growing impact of regulatory innovation. The report offers an in-depth analysis of the chronic disease market in Mainland China, spotlighting five therapies expected to exceed $1 billion in annual sales over the next five years or deliver transformative outcomes for patients. It also explores critical topics shaping global healthcare, including regulatory advancements, the role of radiopharmaceutical theranostics in oncology, and the growing use of real-world data (RWD) and patient-reported outcomes (PROs) to drive health equity and enhance regulatory submissions. Henry Levy, President, Life Sciences & Healthcare, Clarivate, remarked: "Innovation in the life sciences is reaching unprecedented heights, and this year's Drugs to Watch™ report once again demonstrates the industry's ability to deliver therapies that address unmet medical needs and challenge existing paradigms of care. At Clarivate, we take pride in the precision and reliability of our predictions—last year, we identified 13 molecules as Drugs to Watch, with 12 already approved and launched and one poised for launch. This track record reflects the strength of our comprehensive data and deep expertise. By continuing to provide actionable insights, we empower the sector to navigate opportunities, overcome challenges and drive progress in advancing global health." Mike Ward, Global Head of Thought Leadership, Life Sciences & Healthcare, Clarivate, stated: "2025 represents a turning point for the life sciences sector as it embraces cutting-edge technologies such as AI and machine learning to enhance drug discovery and development. This year's report captures the dynamic forces at play, including groundbreaking progress in precision oncology, the rise of radiopharmaceuticals, and the growing focus on addressing global health disparities." The 2025 Drugs to Watch™ report highlights key trends reshaping the life sciences landscape, emphasizing the transformative impact of emerging technologies and therapeutic breakthroughs. Advances in AI and machine learning are streamlining drug discovery, clinical trials, and real-world data integration, enabling precision medicine approaches. The obesity market is undergoing a revolution driven by next-generation GLP-1 therapies, while radiopharmaceutical theranostics are redefining cancer treatment with a "see it and treat it" paradigm. Gene editing technologies are unlocking new opportunities in personalized medicine, and evolving regulatory frameworks are fostering greater emphasis on patient-reported outcomes and health equity. Together, these trends showcase the sector's resilience and its ability to navigate challenges while driving innovation to improve patient care worldwide. This year's drugs to watch exemplify the fusion of innovation and dedication to advancing patient care in an increasingly complex healthcare ecosystem. The Drugs to Watch™ 2025 list include: AWIQLI® (LAI 287; insulin icodec) developed by Novo Nordisk | Type 1 and type 2 diabetes mellitus AWIQLI®, the first once-weekly, subcutaneous insulin, has launched in Australia, Canada, the EU, Mainland China, and Japan. Its weekly dosing offers a significant advantage over daily basal insulin, potentially reducing the treatment burden for patients with type 1 or type 2 diabetes (T1DM and T2DM). CagriSema (cagrilintide + semaglutide) developed by Novo Nordisk | Obesity and type 2 diabetes mellitus CagriSema, combining cagrilintide, a long-acting amylin analog, with semaglutide, promises superior efficacy over semaglutide (OZEMPIC/WEGOVY®) and tirzepatide (MOUNJARO/ZEPBOUND®) in treating obesity and type 2 diabetes. This next-generation GLP-1 therapy leverages the benefits of GLP-1s, such as enhanced insulin secretion and appetite reduction, while incorporating amylin's effects, including slowed glucose absorption and release. If approved, CagriSema will be the first fixed-dose combination of amylin and GLP-1 receptor agonists in the obesity and T2DM markets. COBENFY™ (KarXT; xanomeline-trospium) developed by Bristol Myers Squibb | Schizophrenia and psychosis related to Alzheimer's disease Amid setbacks for emerging schizophrenia treatments, the approval of COBENFY marks a transformative milestone as the first drug in over 30 years with a novel mechanism of action for treating schizophrenia. Combining xanomeline and trospium, COBENFY selectively targets M1 and M4 receptors, rather than traditional dopamine pathways, while minimizing cholinergic side effects. While further data is needed to assess its effectiveness in Alzheimer's disease-related psychosis, COBENFY shows strong commercial potential if proven effective in treating AD-related hallucinations and delusions. EBGLYSS™ (lebrikizumab) developed by Eli Lilly and Co and Almirall | Atopic dermatitis EBGLYSS™, the third biologic targeting IL-13 for atopic dermatitis, follows DUPIXENT® (dupilumab) and ADBRY®/ADTRALZA® (tralokinumab) to market. Its less frequent dosing, more selective IL-13 inhibition, and strong efficacy and safety data position it as a likely first-line treatment for moderate-to-severe atopic dermatitis when topical corticosteroids are inadequate. Fitusiran developed by Alnylam® Pharmaceuticals Inc and Sanofi | Hemophilia A and B Fitusiran, shown to be effective in phase 3 trials for both hemophilia A and B, regardless of inhibitor status, has the potential to offer a new approach to hemophilia treatment. This small interfering RNA (siRNA) therapy works by inhibiting SerpinPC1 mRNA, reducing antithrombin levels, promoting thrombin generation, and helping to rebalance hemostasis to prevent bleeds. Leveraging Alnylam® Pharmaceuticals' ESC-GalNAc conjugate technology, fitusiran could become the first antithrombin-lowering therapy based on a double-stranded RNA molecule, pending approval. GSK-3536819 (MenABCWY) developed by GSK plc | Meningococcus GSK plc's GSK-3536819 vaccine candidate, a 5-in-1, first-generation formulation, targets the five groups of Neisseria meningitidis (A, B, C, W, and Y) responsible for most invasive meningococcal disease (IMD) cases worldwide. It combines the antigenic components of GSK's licensed meningococcal vaccines, BEXSERO (MenB) and MENVEO (MenACWY), both of which have established efficacy and safety profiles. IMDELLTRA™ (tarlatamab-dlle) developed by Amgen | Small-cell lung cancer (SCLC) IMDELLTRA™ is a first-in-class immunotherapy for extensive-stage small cell lung cancer (ES-SCLC). Using Amgen's bispecific T cell engager (BiTE®) molecules, it targets CD3 on T cells and DLL3 on tumor cells, enabling T cells to attack and lyse the tumor. DLL3 is expressed on the surface of SCLC cells in more than 85% of patients but is minimally expressed on healthy cells making it an attractive target. This mechanism positions IMDELLTRA as a potential standard of care for previously treated ES-SCLC. mRESVIA (mRNA-1345) developed by Moderna Inc | RSV With its U.S. FDA approval in May 2024, mRESVIA® joined AREXVY and ABRYSVO, both featured in Drugs to Watch 2024, as respiratory syncytial virus (RSV) vaccines currently available for adults ages 60 years and older, helping further support the public health initiative to reduce the RSV-related disease burden. Even with available vaccines, RSV infections continue to be a public health concern, particularly for infants and older adults (65 years and older). SEL-212 developed by Sobi® and Cartesian Therapeutics Inc/Selecta Biosciences Inc | Gout SEL-212 is a novel, once-monthly treatment combining pegylated uricase (pegadricase; SEL-037) with ImmTOR™, an immune tolerance technology designed to inhibit the formation of anti-drug antibodies (ADAs). For this application, ImmTOR consists of SEL-110.36, an inhibitor of uricase-specific ADA. This approach may help overcome the limitations of reduced efficacy and tolerability seen with other biologic treatments, such as KRYSTEXXA® (pegloticase), in patients with chronic gout. Vepdegestrant (ARV-471) developed by Arvinas Inc and Pfizer Inc | Breast cancer A global collaboration between Arvinas Inc and Pfizer Inc, vepdegestrant may become the first PROteolysis Targeting Chimera (PROTAC®) protein degrader on the market. Designed to target and degrade the estrogen receptor (ER) protein, early studies suggest PROTAC-induced degradation is more complete than with oral selective estrogen receptor degraders (SERDs). This offers potential for overcoming endocrine resistance in breast cancer. Label expansions, including combination with IBRANCE® (palbociclib), are being explored. Zanzalintinib (XL092) developed by Exelixis Inc | Colorectal cancer, renal cell carcinoma and squamous cell carcinoma of head and neck Zanzalintinib is a third-generation oral tyrosine kinase inhibitor targeting VEGF receptors, MET, and TAM kinases involved in tumor growth and immunosuppression. Currently in phase 3 trials for non-clear-cell renal cell carcinoma (nccRCC), colorectal cancer (CRC) and squamous cell carcinoma of the head and neck (SCCHN), the company anticipates one potential zanzalintinib launch per year starting as early as 2026. Compared to CABOMETYX® (cabozantinib), zanzalintinib may offer benefits, including approval for nccRCC histology and a broader patient population. Access the Drugs to Watch 2025 report from Clarivate, here. For more Drugs to Watch updates and analyses throughout the year, visit the Drugs to Watch web page and follow Clarivate for Life Sciences & Healthcare on LinkedIn and X. Join the conversation, using #DrugstoWatch. To learn more about how Clarivate can help healthcare companies inform and shape the drug discovery, development and delivery process, visit here. Methodology for the Clarivate Drugs to Watch 2025 Report To identify this year's Drugs to Watch, Clarivate drew from the expertise of over 160 analysts covering hundreds of diseases, drugs and markets, along with 11 integrated data sets that span the R&D and commercialization lifecycle, including: Cortellis Competitive Intelligence™, Disease Landscape & Forecast, Epidemiology Intelligence, BioWorld™, Cortellis Regulatory Intelligence™, Drug Timeline & Success Rates, Cortellis Clinical Trials Intelligence™, Cortellis Deals Intelligence™, Access & Reimbursement payer studies, Clarivate Real-World Data and Analytics, Web of Science™, Derwent Innovation™, and other industry sources including biopharma company press releases, filings and peer-reviewed publications. Candidate drugs in phase 2 or phase 3 trials, at pre-registration or registration stage, or already launched in 2024 were selected for analysis, including both novel treatments and already-marketed drugs pursuing new indications that could be particularly impactful. Drugs launched prior to 2024 were excluded. The dataset was filtered for drugs that had total forecast sales of $1 billion or more by 2030. Clarivate experts and analysts evaluated each drug in its individual context, based on factors such as expected approval or launch dates, competitive landscape, regulatory status, trial results, market dynamics and other key factors, and added novel drugs that, while likely to fall short of blockbuster status, are poised to be therapeutic game-changers. Please note that Clarivate analysts generated the data shown in this report prior to December 31, 2024. The Drugs to Watch 2025 Report and the treatments referenced in this release are based on Clarivate's current expectations per existing data, but actual results derived from the drugs named in the report and here may differ significantly. Clarivate is committed to comprehensively supporting customers across the entire drug, device and medical technology lifecycles to advance human health. By combining patient journey data, therapeutic area expertise, artificial intelligence and analytics in ways that unlock hidden insights, data-driven decisions and accelerating innovation, Clarivate's end-to-end research intelligence is designed to enable customers to make informed evidence-based decisions. About Clarivate Clarivate™ is a leading global provider of transformative intelligence. We offer enriched data, insights & analytics, workflow solutions and expert services in the areas of Academia & Government, Intellectual Property and Life Sciences & Healthcare. For more information, please visit . Media Contact: Catherine Daniel Director, External Communications, Life Sciences & Healthcare [email protected] SOURCE Clarivate Plc WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM? 440k+ Newsrooms & Influencers 9k+ Digital Media Outlets 270k+ Journalists Opted In GET STARTED

VaccinePhase 3Immunotherapy

06 Jan 2025

·www.businesswire.com

Exelixis to Present at the 43rd Annual J.P. Morgan Healthcare Conference on January 13, 2025

ALAMEDA, Calif.--( BUSINESS WIRE )--Exelixis, Inc. (Nasdaq: EXEL) today announced that Michael M. Morrissey, Ph.D., the company’s President and Chief Executive Officer, will provide a corporate overview at the 43 rd Annual J.P. Morgan Healthcare Conference on Monday, January 13, 2025 at 5:15 p.m. PT / 8:15 p.m. PT. To access the webcast link, log onto www.exelixis.com and proceed to the Event Calendar page under the Investors & News heading. Replays will also be available at the same location for at least 30 days. About Exelixis Exelixis is a globally ambitious oncology company innovating next-generation medicines and regimens at the forefront of cancer care. Powered by drug discovery and development excellence, we are rapidly evolving our product portfolio to target an expanding range of tumor types and indications with our clinically differentiated pipeline of small molecules, antibody-drug conjugates and other biotherapeutics. This comprehensive approach harnesses decades of robust investment in our science and partnerships to advance our investigational programs and extend the impact of our flagship commercial product, CABOMETYX ® (cabozantinib). Exelixis is driven by a bold scientific pursuit to create transformational treatments that give more patients hope for the future. For information about the company and its mission to help cancer patients recover stronger and live longer, visit www.exelixis.com , follow @ExelixisInc on X (Twitter), like Exelixis, Inc. on Facebook and follow Exelixis on LinkedIn. Exelixis, the Exelixis logo and CABOMETYX are registered U.S. trademarks.

100 Deals associated with Cabozantinib (s)-Malate

External Link

KEGG	Wiki	ATC	Drug Bank
D10095	Cabozantinib (s)-Malate	L01XE26	DB08875

R&D Status

Approved

10 top approved records.

to view more data

Indication	Country/Location	Organization	Date
Thyroid Cancer	US	Exelixis, Inc.	17 Sep 2021
Differentiated Thyroid Gland Carcinoma	KR	Ipsen Ltd.	26 Sep 2017
Renal Cell Carcinoma	KR	Ipsen Ltd.	26 Sep 2017
Hepatocellular Carcinoma	EU	Ipsen Pharma SAS	09 Sep 2016
Hepatocellular Carcinoma	IS	Ipsen Pharma SAS	09 Sep 2016
Hepatocellular Carcinoma	LI	Ipsen Pharma SAS	09 Sep 2016
Hepatocellular Carcinoma	NO	Ipsen Pharma SAS	09 Sep 2016
Advanced Renal Cell Carcinoma	US	Exelixis, Inc.	25 Apr 2016
Thyroid Cancer, Medullary	US	Exelixis, Inc.	29 Nov 2012

Developing

10 top R&D records.

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Neuroendocrine tumor of pancreas	NDA/BLA	US	Exelixis, Inc.	06 Aug 2024
Solid tumor	NDA/BLA	CN	Jiangsu Hansoh Pharmaceutical Co., Ltd.	28 Sep 2020
Refractory Differentiated Thyroid Gland Carcinoma	Phase 3	US	National Cancer Institute	22 Aug 2024
Metastatic osteosarcoma	Phase 3	-	National Cancer Institute	13 Jan 2023
Unresectable Bone Sarcoma	Phase 3	-	National Cancer Institute	13 Jan 2023
Advanced Urothelial Carcinoma	Phase 3	US	National Cancer Institute	03 Jun 2022
Advanced Urothelial Carcinoma	Phase 3	CA	National Cancer Institute	03 Jun 2022
Bladder Cancer	Phase 3	US	National Cancer Institute	03 Jun 2022
Bladder Cancer	Phase 3	CA	National Cancer Institute	03 Jun 2022
Metastatic Urethral Urothelial Carcinoma	Phase 3	US	National Cancer Institute	03 Jun 2022

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


JPRN-jRCT1080224637 (ASCO_GI2025)	Phase 1/2	Metastatic Colorectal Carcinoma MET amplification \| RAS \| BRAF	35	Cabozantinib	ckymeswxvx(hodksfoplr) = iarhenbhua vtjmiqaxxk (cbxzrsukdr, 0.2 - 36) View more	Negative	23 Jan 2025
				Panitumumab	acwojhlnli(dwharbuekk) = mciwspkbkw jdsjcaexin (udzodmcwot )
NCT03375320 (CABINET, ASCO_GI2025)	Phase 3	Gastro-Enteropancreatic Neuroendocrine Tumor	203	Cabozantinib 60 mg daily	gqzytgpwih(ankezdfsjq) = wkuamejbiy hnlqqcifyb (etlvavwjfp, 6.0 - 16.7) View more	Positive	23 Jan 2025
				Placebo	gqzytgpwih(ankezdfsjq) = szeiywzqxr hnlqqcifyb (etlvavwjfp, 3.9 - 11.0)
NCT04963283 (ASCO_GI2025)	Phase 2	Metastatic Microsatellite Stable Colorectal Carcinoma	49	Cabozantinib 40 mg	xxzmasvrzq(sjogimtebw) = dvsftbmamp zzkfbjegvs (tvddksprrr, 0.264 - 0.557) View more	Positive	23 Jan 2025
NCT03468218 (CTgov)	Phase 2	Squamous cell carcinoma of the paranasal sinus \| Squamous cell carcinoma of the oral cavity recurrent \| Squamous Cell Carcinoma of the Oropharynx ... View more	36	Cabozantinib+pembrolizumab	dskuenabdp(qpvsrzwiwd) = kdqdoiyxhy ewnumbjnjl (gnlpqagpku, sqkplfnvgx - lfaybcfbon) View more	-	27 Dec 2024
NCT03945773 (CaboPoint, CTgov)	Phase 2	Metastatic Renal Cell Carcinoma \| Locally Advanced Renal Cell Carcinoma \| Metastatic Clear Cell Renal Cell Carcinoma	127	Cabozantinib (Cohort A)	ljjpqxrzue(hnsunbdfot) = dsoykyrolg dfdvatlwxb (zlmkluiarq, fxzjvhdiwq - hupdgafhmf) View more	-	19 Dec 2024
				Cabozantinib (Cohort B)	fyoahtbefk(mgzjhjtqek) = lgihngbubc gyfcburkih (tnzhxondcz, ehhvfmbgqy - muqxikvkvw) View more
NCT03370718 (SAT-175, CTgov)	Phase 2	Adrenocortical Carcinoma	18	Cabozantinib	vvwpkxwgnm(bmntqrztiy) = hkykhewmfq ydjlurtghw (ukfugnkiwr, hkupnqibjb - kfwnmpwlqh) View more	-	10 Dec 2024
ESMO_ASIA2024 Manual	Not Applicable	Advanced Renal Cell Carcinoma First line	41	Cabozantinib plus Nivolumab	wkznjjlkqp(cydozifkab) = wikzngptyc tupsekxuuz (qqwxgthlae ) View more	Positive	07 Dec 2024
				Cabozantinib	wkznjjlkqp(cydozifkab) = gjmejflapu tupsekxuuz (qqwxgthlae ) View more
NCT04091750 (CTgov)	Phase 2	Unresectable Melanoma	14	ipilimumab+Nivolumab+Cabozantinib	xwacgudecf(yngcodvtfb) = msvaxpzqem ltbpgqqyle (bbjvexeqne, qxwvkuwlqm - nyjaxxkpgk) View more	-	27 Nov 2024
NCT03534804 (PemCab, CTgov)	Phase 2	Advanced Urothelial Carcinoma \| Bladder Cancer \| Metastatic urothelial carcinoma	37	Cabozantinib+pembrolizumab	avlleuxnzu(lkhrjnyhtl) = wcwwpyvbas bsmbcewgzv (oruexsihgn, jhoyqcpbrh - zpjghmuqqq) View more	-	26 Nov 2024
NCT03375320 (CABINET \| A021602, CTgov)	Phase 3	Well Differentiated Pancreatic Endocrine Tumor \| Neuroendocrine tumor of pancreas \| Carcinoid Tumor ... View more	298	Cabozantinib S-malate (Arm Ia (Cabozantinib S-malate, Extra-pancreatic NET Cohort [epNET]))	knazmuibxv(mjsrcmgxlx) = vnfkslubhc zcsvrjibvs (sjrzrgidrg, xeoakujmvq - grvlywdwia) View more	-	16 Oct 2024
				Placebo (Arm IIa (Placebo, Extra-pancreatic NET Cohort [epNET]))	knazmuibxv(mjsrcmgxlx) = qwfirgtgoy zcsvrjibvs (sjrzrgidrg, lvyeymnsfi - ipmwopoyjo) View more

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