Advanced Renal Cell Carcinoma

Also known as: Advanced Renal cell carcinoma

DrugDrug NameDrug Description
DB08875CabozantinibCabozantinib was approved in 2012 and is a non-specific tyrosine kinase inhibitor. It is marketed as Cometriq, which is indicated for the treatment of metastatic medullary thyroid cancer. It's label includes a black box warning of gastrointestinal perforations, fistulas, and hemorrhage. The FDA approved cabozantinib as Cabometyx for patients with advanced renal cell carcinoma in April 2016.
DB06186IpilimumabIpilimumab is a monoclonal antibody, more specifically a fully humanized IgG1 antibody produced in mammalian cell culture, to the cytotoxic T lymphocyte antigen-4 (CTLA-4) which activates antitumor immunity by inhibiting this major checkpoint.[A35065, A35080] This antineoplastic agent was developed by Bristol-Myers Squibb and Medarex and FDA approved on March 25, 2011, for the treatment of melanoma.[L3581] On October 2015, the FDA approved expanded the indications for Ipilimumab, allowing it to be used to reduce the risk of relapsed skin cancer after surgery.[L3582] On July 11, 2018, the FDA approved an additional indication for the combination of low dose ipilimumab and [nivolumab] for the treatment of previously treated microsatellite instability-high/deficient mismatch repair (MSI-H/dMMR) metastatic colorectal cancer.[L3590]
DB09078LenvatinibLenvatinib is a receptor tyrosine kinase (RTK) inhibitor that inhibits the kinase activities of vascular endothelial growth factor (VEGF) receptors VEGFR1 (FLT1), VEGFR2 (KDR), and VEGFR3 (FLT4). Lenvatinib also inhibits other RTKs that have been implicated in pathogenic angiogenesis, tumor growth, and cancer progression in addition to their normal cellular functions, including fibroblast growth factor (FGF) receptors FGFR1, 2, 3, and 4; the platelet derived growth factor receptor alpha (PDGFRα), KIT, and RET. These receptor tyrosine kinases (RTKs) located in the cell membrane play a central role in the activation of signal transduction pathways involved in the normal regulation of cellular processes, such as cell proliferation, migration, apoptosis and differentiation, and in pathogenic angiogenesis, lymphogenesis, tumour growth and cancer progression. In particular, VEGF has been identified as a crucial regulator of both physiologic and pathologic angiogenesis and increased expression of VEGF is associated with a poor prognosis in many types of cancers. Lenvatinib is indicated for the treatment of patients with locally recurrent or metastatic, progressive, radioactive iodine (RAI)-refractory differentiated thyroid cancer. Most patients with thyroid cancer have a very good prognosis with treatment (98% 5 year survival rate) involving surgery and hormone therapy. However, for patients with RAI-refractory thyroid cancer, treatment options are limited and the prognosis is poor, leading to a push for the development of more targeted therapies such as lenvatinib.
DB06589PazopanibPazopanib is a small molecule inhibitor of multiple protein tyrosine kinases with potential antineoplastic activity. It is developed by GlaxoSmithKline and was FDA approved on October 19, 2009.
DB00398SorafenibSorafenib (rINN), marketed as Nexavar by Bayer, is a drug approved for the treatment of advanced renal cell carcinoma (primary kidney cancer). It has also received "Fast Track" designation by the FDA for the treatment of advanced hepatocellular carcinoma (primary liver cancer), and has since performed well in Phase III trials. Sorafenib is a small molecular inhibitor of Raf kinase, PDGF (platelet-derived growth factor), VEGF receptor 2 & 3 kinases and c Kit the receptor for Stem cell factor. A growing number of drugs target most of these pathways. The originality of Sorafenib lays in its simultaneous targeting of the Raf/Mek/Erk pathway.
DB01268SunitinibSunitinib is a small-molecule multi-targeted receptor tyrosine kinase (RTK) inhibitor. On January 26, 2006, the agent was formally approved by the US FDA for the indications of treating renal cell carcinoma (RCC) and imatinib-resistant gastrointestinal stromal tumor (GIST). For these purposes, sunitinib is generally available as an orally administered formulation. Sunitinib inhibits cellular signaling by targeting multiple RTKs. These include all platelet-derived growth factor receptors (PDGF-R) and vascular endothelial growth factor receptors (VEGF-R). Sunitinib also inhibits KIT (CD117), the RTK that drives the majority of GISTs. In addition, sunitinib inhibits other RTKs including RET, CSF-1R, and flt3.
DB06287TemsirolimusTemsirolimus is a derivative of sirolimus used in the treatment of renal cell carcinoma (RCC). It was developed by Wyeth Pharmaceuticals under the trade name Torisel. Temsirolimus was approved by the FDA in late May 2007 as well as the European Medicines Agency (EMEA) on November 2007.
DrugDrug NameTargetType
DB08875CabozantinibCytochrome P450 3A4enzyme
DB08875CabozantinibCytochrome P450 2C9enzyme
DB08875CabozantinibHepatocyte growth factor receptortarget
DB08875CabozantinibVascular endothelial growth factor receptor 2target
DB08875CabozantinibProto-oncogene tyrosine-protein kinase receptor Rettarget
DB08875CabozantinibCytochrome P450 2C8enzyme
DB06186IpilimumabCytotoxic T-lymphocyte protein 4target
DB09078LenvatinibVascular endothelial growth factor receptor 1target
DB09078LenvatinibVascular endothelial growth factor receptor 2target
DB09078LenvatinibVascular endothelial growth factor receptor 3target
DB09078LenvatinibFibroblast growth factor receptor 1target
DB09078LenvatinibFibroblast growth factor receptor 2target
DB09078LenvatinibFibroblast growth factor receptor 3target
DB09078LenvatinibFibroblast growth factor receptor 4target
DB09078LenvatinibPlatelet derived growth factor receptor alphatarget
DB09078LenvatinibRETtarget
DB09078LenvatinibMast/stem cell growth factor receptor Kittarget
DB09078LenvatinibMultidrug resistance protein 1transporter
DB09078LenvatinibATP-binding cassette sub-family G member 2transporter
DB09078LenvatinibCytochrome P450 3A4enzyme
DB09078LenvatinibAldehyde oxidaseenzyme
DB09078LenvatinibCytochrome P450 2C8enzyme
DB09078LenvatinibCytochrome P450 2C9enzyme
DB09078LenvatinibCytochrome P450 1A2enzyme
DB09078LenvatinibCytochrome P450 2B6enzyme
DB09078LenvatinibCytochrome P450 2C19enzyme
DB09078LenvatinibSolute carrier family 22 member 6transporter
DB09078LenvatinibSolute carrier family 22 member 8transporter
DB09078LenvatinibSolute carrier family 22 member 2transporter
DB09078LenvatinibSolute carrier organic anion transporter family member 1B1transporter
DB09078LenvatinibBile salt export pumptransporter
DB09078LenvatinibCytochrome P450 2D6enzyme
DB06589PazopanibVascular endothelial growth factor receptor 1target
DB06589PazopanibVascular endothelial growth factor receptor 2target
DB06589PazopanibVascular endothelial growth factor receptor 3target
DB06589PazopanibPlatelet-derived growth factor receptor alphatarget
DB06589PazopanibPlatelet-derived growth factor receptor betatarget
DB06589PazopanibMast/stem cell growth factor receptor Kittarget
DB06589PazopanibCytochrome P450 3A4enzyme
DB06589PazopanibCytochrome P450 2D6enzyme
DB06589PazopanibCytochrome P450 2C8enzyme
DB06589PazopanibCytochrome P450 1A2enzyme
DB06589PazopanibMultidrug resistance protein 1transporter
DB06589PazopanibATP-binding cassette sub-family G member 2transporter
DB06589PazopanibSolute carrier organic anion transporter family member 1B1transporter
DB06589PazopanibUDP-glucuronosyltransferase 1-1transporter
DB06589PazopanibFibroblast growth factor receptor 3target
DB06589PazopanibTyrosine-protein kinase ITK/TSKtarget
DB06589PazopanibFibroblast growth factor 1target
DB06589PazopanibSH2B adapter protein 3target
DB00398SorafenibSerine/threonine-protein kinase B-raftarget
DB00398SorafenibReceptor-type tyrosine-protein kinase FLT3target
DB00398SorafenibRAF proto-oncogene serine/threonine-protein kinasetarget
DB00398SorafenibVascular endothelial growth factor receptor 3target
DB00398SorafenibPlatelet-derived growth factor receptor betatarget
DB00398SorafenibMast/stem cell growth factor receptor Kittarget
DB00398SorafenibVascular endothelial growth factor receptor 2target
DB00398SorafenibCytochrome P450 3A4enzyme
DB00398SorafenibUDP-glucuronosyltransferase 1-9enzyme
DB00398SorafenibCytochrome P450 2B6enzyme
DB00398SorafenibCytochrome P450 2C8enzyme
DB00398SorafenibCytochrome P450 3A5enzyme
DB00398SorafenibCytochrome P450 3A7enzyme
DB00398SorafenibCytochrome P450 2C9enzyme
DB00398SorafenibMultidrug resistance-associated protein 4transporter
DB00398SorafenibMultidrug resistance protein 1transporter
DB00398SorafenibCanalicular multispecific organic anion transporter 1transporter
DB00398SorafenibATP-binding cassette sub-family G member 2transporter
DB00398SorafenibCytochrome P450 1A2enzyme
DB00398SorafenibCytochrome P450 2C19enzyme
DB00398SorafenibCytochrome P450 2D6enzyme
DB00398SorafenibUDP-glucuronosyltransferase 1-1enzyme
DB00398SorafenibRalA-binding protein 1transporter
DB00398SorafenibFibroblast growth factor receptor 1target
DB00398SorafenibProto-oncogene tyrosine-protein kinase receptor Rettarget
DB00398SorafenibVascular endothelial growth factor receptor 1target
DB00398SorafenibSolute carrier organic anion transporter family member 1B1transporter
DB01268SunitinibPlatelet-derived growth factor receptor betatarget
DB01268SunitinibVascular endothelial growth factor receptor 1target
DB01268SunitinibVascular endothelial growth factor receptor 2target
DB01268SunitinibVascular endothelial growth factor receptor 3target
DB01268SunitinibMast/stem cell growth factor receptor Kittarget
DB01268SunitinibReceptor-type tyrosine-protein kinase FLT3target
DB01268SunitinibMacrophage colony-stimulating factor 1 receptortarget
DB01268SunitinibPlatelet-derived growth factor receptor alphatarget
DB01268SunitinibCytochrome P450 3A4enzyme
DB01268SunitinibCytochrome P450 3A5enzyme
DB01268SunitinibCytochrome P450 3A7enzyme
DB01268SunitinibMultidrug resistance-associated protein 4transporter
DB01268SunitinibMultidrug resistance protein 1transporter
DB01268SunitinibCanalicular multispecific organic anion transporter 1transporter
DB01268SunitinibATP-binding cassette sub-family G member 2transporter
DB06287TemsirolimusSerine/threonine-protein kinase mTORtarget
DB06287TemsirolimusCytochrome P450 3A4enzyme
DB06287TemsirolimusCytochrome P450 3A5enzyme
DB06287TemsirolimusCytochrome P450 3A7enzyme
DB06287TemsirolimusCytochrome P450 2D6enzyme
DB06287TemsirolimusMultidrug resistance protein 1transporter
DrugDrug NamePhaseStatusCount
DB06091Evofosfamide1Unknown Status1
DB06186Ipilimumab1Recruiting1
DB09035Nivolumab1Recruiting1
DB12665Isoquercetin1 / 2Recruiting1
DB06589Pazopanib1 / 2Active Not Recruiting1
DB01268Sunitinib1 / 2Recruiting1
DB06080ABT-8692Completed1
DB06626Axitinib2Completed1
DB08875Cabozantinib2Active Not Recruiting1
DB08875Cabozantinib2Recruiting1
DB06186Ipilimumab2Recruiting1
DB09035Nivolumab2Recruiting1
DB01269Panitumumab2Completed2
DB06589Pazopanib2Recruiting1
DB00398Sorafenib2Completed1
DB01268Sunitinib2Active Not Recruiting1
DB15232Telaglenastat2Recruiting1
DB06287Temsirolimus2Completed1
DB12056Trebananib2Active Not Recruiting1
DB12056Trebananib2Completed1
DB06186Ipilimumab3Active Not Recruiting1
DB09035Nivolumab3Active Not Recruiting1
DB00398Sorafenib3Completed2
DB01268Sunitinib3Active Not Recruiting1
DB01268Sunitinib3Terminated1
DB11800Tivozanib3Completed2
DB06626AxitinibNot AvailableRecruiting1