Unresectable Melanoma

DrugDrug NameDrug Description
DB05239CobimetinibCobimetinib is an orally active, potent and highly selective small molecule inhibiting mitogen-activated protein kinase kinase 1 (MAP2K1 or MEK1), and central components of the RAS/RAF/MEK/ERK signal transduction pathway. It has been approved in Switzerland and the US, in combination with vemurafenib for the treatment of patients with unresectable or metastatic BRAF V600 mutation-positive melanoma.
DB08912DabrafenibDabrafenib mesylate is a reversible ATP-competitive kinase inhibitor and targets the MAPK pathway. FDA approved on May 29, 2013.
DB06186IpilimumabIpilimumab, a recombinant human monoclonal antibody (IgG1 kappa immunoglobin), is an antineoplastic agent developed by Bristol-Myers Squibb and Medarex for the treatment of unresectable or metastatic melanoma in adults. Ipilimumab received FDA approved on March 25, 2011. In October 2015, the FDA approved expanded the indications for Ipilimumab, allowing it to be used to reduce the risk of the deadly skin cancer returning after surgery.
DB09035NivolumabNivolumab is a fully human IgG4 monoclonal antibody that acts as an immunomodulator by blocking ligand activation of programmed cell death 1 (PD-1) receptor on T cells. It is indicated for use in patients with unresectable (cannot be surgically removed) or metastatic melanoma who no longer respond to other drugs. Nivolumab is administered as an intravenous infusion over 60 minutes every 2 weeks.
DB09037PembrolizumabPembrolizumab is a humanized monoclonal antibody that blocks the interaction between PD-1 and its ligands, PD-L1 and PD-L2. It is used for the treatment of several types of cancer such as, Melanoma, Non-Small Cell Lung Cancer and Head and Neck Cancer. Due to its success in clinical trials, pembrolizumab was approved early to allow quick patient access and was given breakthrough therapy and orphan drug designation. Pembrolizumab (as Keytruda) was approved by the U.S. Food and Drug Administration to treat advanced cases of the most common type of lung malignancy, non-small cell lung cancer on Oct. 2, 2015. Keytruda was additionally approved for the treatment of Classical Hodgkin Lymphoma (cHL) in March, 2017.
DB08911TrametinibTrametinib dimethyl sulfoxide is a kinase inhibitor. Each 1-mg tablet contains 1.127 mg trametinib dimethyl sulfoxide equivalent to 1 mg of trametinib non-solvated parent. FDA approved on May 29, 2013.
DB08881VemurafenibVemurafenib is a competitive kinase inhibitor with activity against BRAF kinase with mutations like V600E.[A31269] It exerts its function by binding to the ATP-binding domain of the mutant BRAF.[A31270] Vemurafenib was co-developed by Roche and Plexxikon and it obtained its FDA approval on August 17, 2011, under the company Hoffmann La Roche. After approval, Roche in collaboration with Genentech launched a broad development program. [L1012]
DrugDrug NameTargetType
DB05239CobimetinibDual specificity mitogen-activated protein kinase kinase 1target
DB05239CobimetinibCYP3Aenzyme
DB05239CobimetinibMultidrug resistance protein 1enzyme
DB05239CobimetinibSolute carrier organic anion transporter family member 1B1transporter
DB05239CobimetinibSolute carrier organic anion transporter family member 1B3transporter
DB05239CobimetinibATP-binding cassette sub-family G member 2transporter
DB08912DabrafenibCytochrome P450 3A4enzyme
DB08912DabrafenibCytochrome P450 2C8enzyme
DB08912DabrafenibMultidrug resistance protein 1transporter
DB08912DabrafenibATP-binding cassette sub-family G member 2transporter
DB08912DabrafenibSolute carrier organic anion transporter family member 1B1transporter
DB08912DabrafenibSolute carrier organic anion transporter family member 1B3transporter
DB08912DabrafenibSolute carrier family 22 member 6transporter
DB08912DabrafenibSolute carrier family 22 member 8transporter
DB08912DabrafenibSerine/threonine-protein kinase B-raftarget
DB08912DabrafenibRAF proto-oncogene serine/threonine-protein kinasetarget
DB08912DabrafenibSerine/threonine-protein kinase SIK1target
DB08912DabrafenibSerine/threonine-protein kinase Nek11target
DB08912DabrafenibLIM domain kinase 1target
DB06186IpilimumabCytotoxic T-lymphocyte protein 4target
DB09035NivolumabProgrammed cell death protein 1target
DB09037PembrolizumabProgrammed cell death protein 1target
DB08911TrametinibCytochrome P450 2C8enzyme
DB08911TrametinibCytochrome P450 3A4enzyme
DB08911TrametinibDual specificity mitogen-activated protein kinase kinase 1target
DB08911TrametinibDual specificity mitogen-activated protein kinase kinase 2target
DB08881VemurafenibSerum albumincarrier
DB08881VemurafenibAlpha-1-acid glycoprotein 1carrier
DB08881VemurafenibCytochrome P450 1A2enzyme
DB08881VemurafenibCytochrome P450 2D6enzyme
DB08881VemurafenibCytochrome P450 3A4enzyme
DB08881VemurafenibSerine/threonine-protein kinase B-raftarget
DB08881VemurafenibMultidrug resistance-associated protein 1transporter
DB08881VemurafenibATP-binding cassette sub-family G member 2transporter
DrugDrug NamePhaseStatusCount
DB06186Ipilimumab1Completed1
DB08912Dabrafenib2Active Not Recruiting1
DB06186Ipilimumab2Active Not Recruiting1
DB09035Nivolumab2Active Not Recruiting1
DB01229Paclitaxel2Active Not Recruiting1
DB06589Pazopanib2Active Not Recruiting1