EXEL
Exelixis is an oncology company with four marketed products including cabozantinib, a small molecule tyrosine kinase inhibitor approved across multiple cancer indications including renal cell carcinoma, hepatocellular carcinoma, thyroid cancer, and pancreatic neuroendocrine tumors, along with cobimetinib for melanoma and esaxerenone for hypertension. The company's lead late-stage program is zanzalintinib, a novel oral kinase inhibitor currently under FDA review for colorectal cancer with an extensive development program spanning multiple oncology indications including renal cell carcinoma, neuroendocrine tumors, and meningioma. Exelixis is advancing a diverse pipeline of phase 1 programs including XL309 (small molecule USP1 inhibitor), XB010 (antibody-drug conjugate targeting 5T
Pipeline
Abiraterone acetate is converted in vivo to abiraterone, an androgen biosynthesis inhibitor, that inhibits 17 α-hydroxylase/C17,20-lyase (CYP17). This enzyme is expressed in testicular, adrenal, and prostatic tumor tissues and is required for androgen biosynthesis.
Anti-PD-L1 monoclonal antibody (Tecentriq) that blocks PD-L1, restoring T-cell anti-tumor activity. Approved in NSCLC, SCLC, urothelial, and hepatocellular carcinoma.
Oral multi-kinase inhibitor (Cabometyx) targeting VEGFR2, MET, and AXL. Approved in renal cell carcinoma, hepatocellular carcinoma, and differentiated thyroid cancer.
Oral second-generation androgen receptor antagonist (Xtandi) that blocks AR signaling. Approved in metastatic and non-metastatic castration-resistant prostate cancer.
Anti-CTLA-4 monoclonal antibody (Yervoy) that releases T-cell inhibition early in immune activation. Approved in melanoma, RCC, MSI-H colorectal, and other cancers, often combined with nivolumab.
Anti-PD-1 monoclonal antibody (Opdivo) that blocks the PD-1 checkpoint. Approved across melanoma, NSCLC, RCC, head and neck, hepatocellular, and other cancers.
Oral synthetic corticosteroid used as anti-inflammatory and immunosuppressant. Backbone in lymphoma regimens (R-CHOP, BEACOPP) and supportive care.
Regorafenib is a small molecule inhibitor of multiple membrane-bound and intracellular kinases involved in normal cellular functions and in pathologic processes such as oncogenesis, tumor angiogenesis, metastasis and tumor immunity.
Sunitinib is a small molecule that inhibits multiple receptor tyrosine kinases (RTKs), some of which are implicated in tumor growth, pathologic angiogenesis, and metastatic progression of cancer.
Everolimus is an inhibitor of mammalian target of rapamycin (mTOR), a serine-threonine kinase, downstream of the PI3K/AKT pathway. The mTOR pathway is dysregulated in several human cancers and in tuberous sclerosis complex (TSC).
Anti-PD-1 monoclonal antibody (Keytruda) that blocks the PD-1 checkpoint, restoring anti-tumor immune response. FDA-approved across many cancers including NSCLC, melanoma, and gastroesophageal cancer.