Metastatic Melanoma

Also known as: Malignant melanoma, metastatic / Metastatic malignant melanoma

DrugDrug NameDrug Description
DB00041AldesleukinAldesleukin, a lymphokine, is produced by recombinant DNA technology using a genetically engineered E. coli strain containing an analog of the human interleukin-2 gene. Genetic engineering techniques were used to modify the human IL-2 gene, and the resulting expression clone encodes a modified human interleukin-2. This recombinant form differs from native interleukin-2 in the following ways: a) Aldesleukin is not glycosylated because it is derived from E. coli; b) the molecule has no N-terminal alanine; the codon for this amino acid was deleted during the genetic engineering procedure; c) the molecule has serine substituted for cysteine at amino acid position 125.
DB11967BinimetinibBinimetinib, also known as _Mektovi_, is a potent is a potent and selective oral mitogen-activated protein kinase 1/2 (MEK 1/2) inhibitor which is combined with [Encorafenib] [A34275],[L3335]. On June 27, 2018, the Food and Drug Administration approved the combination of [Encorafenib] and binimetinib (BRAFTOVI and MEKTOVI, from Array BioPharma Inc.) in combination for patients with unresectable or metastatic melanoma with the BRAF V600E or V600K mutations, as detected by an FDA-approved test [L3335].
DB00515CisplatinCisplatin, cisplatinum or cis-diamminedichloroplatinum(II) (CDDP) is a platinum-based chemotherapy drug used to treat various types of cancers, including sarcomas, some carcinomas (e.g. small cell lung cancer, and ovarian cancer), lymphomas and germ cell tumors. It was the first member of its class, which now also includes carboplatin and oxaliplatin.
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 (Tafinlar) is a reversible ATP-competitive kinase inhibitor and targets the MAPK pathway. It was approved on May 29, 2013 for the treatment of melanoma [L2718]. In May 2018, Tafinlar (dabrafenib) and Mekinist ([DB08911]) in combination have been approved to treat anaplastic thyroid cancer caused by an abnormal BRAF V600E gene [L2714].
DB00851DacarbazineAn antineoplastic agent. It has significant activity against melanomas. (from Martindale, The Extra Pharmacopoeia, 31st ed, p564). Dacarbazine with Oblimersen is in clinical trials for the treatment of malignant melanoma.
DB11718EncorafenibEncorafenib, also known as _BRAFTOVI_, is a kinase inhibitor. Encorafenib inhibits BRAF gene, which encodes for B-raf protein, which is a proto-oncogene involved in various genetic mutations [FDA label]. This protein plays a role in regulating the MAP kinase/ERK signaling pathway, which impacts cell division, differentiation, and secretion. Mutations in this gene, most frequently the V600E mutation, are the most commonly identified cancer-causing mutations in melanoma, and have been isolated in various other cancers as well, including non-Hodgkin lymphoma, colorectal cancer, thyroid carcinoma, non-small cell lung carcinoma, hairy cell leukemia and adenocarcinoma of the lung [L3344]. On June 27, 2018, the Food and Drug Administration approved encorafenib and [Binimetinib] (BRAFTOVI and MEKTOVI, Array BioPharma Inc.) in combination for patients with unresectable or metastatic melanoma with a BRAF V600E or V600K mutation, as detected by an FDA-approved test [FDA label].
DB00619ImatinibImatinib is a small molecule kinase inhibitor used to treat certain types of cancer. It is currently marketed by Novartis as Gleevec (USA) or Glivec (Europe/Australia) as its mesylate salt, imatinib mesilate (INN). It is occasionally referred to as CGP57148B or STI571 (especially in older publications). It is used in treating chronic myelogenous leukemia (CML), gastrointestinal stromal tumors (GISTs) and a number of other malignancies. It is the first member of a new class of agents that act by inhibiting particular tyrosine kinase enzymes, instead of non-specifically inhibiting rapidly dividing cells.
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]
DB09035NivolumabNivolumab is a fully humanized IgG4 antibody targeting the immune checkpoint programmed death receptor-1 (PD-1). This molecule was produced entirely on mice and grafted onto human kappa and IgG4 Fc region with the mutation _S228P_ for additional stability and reduced variability.[A35203] It is developed by Bristol Myers Squibb and originally FDA approved on December 22, 2014. Since this approval, nivolumab has been approved for a variety of other uses related to cancer therapy. On 2017, was notably approved for the treatment of hepatocellular carcinoma[L3632] and on July 11, 2018, the FDA approved this agent in combination with low doses of [ipilimumab] for the treatment of MSI-H/dMMR metastatic colorectal cancer.[L3611]
DB01229PaclitaxelPaclitaxel is a mitotic inhibitor used in cancer chemotherapy. It was discovered in a US National Cancer Institute program at the Research Triangle Institute in 1967 when Monroe E. Wall and Mansukh C. Wani isolated it from the bark of the Pacific yew tree, Taxus brevifolia and named it taxol. Later it was discovered that endophytic fungi in the bark synthesize paclitaxel. When it was developed commercially by Bristol-Myers Squibb (BMS), the generic name was changed to paclitaxel and the BMS compound is sold under the trademark Taxol. In this formulation, paclitaxel is dissolved in Kolliphor EL and ethanol, as a delivery agent. A newer formulation, in which paclitaxel is bound to albumin, is sold under the trademark Abraxane. [Wikipedia]
DB09037PembrolizumabPembrolizumab is a highly selective IgG4-kappa humanized monoclonal antibody against PD-1 receptor. It was generated by grafting the variable sequences of a very high-affinity mouse antihuman PD-1 antibody onto a human IgG4-kappa isotype with the containing a stabilizing S228P Fc mutation.[A18829] It contains 32 cysteine residues and the complete folded molecule includes 4 disulfide linkages as interchain bonds and 23 interchain bonds.[F136] It was developed by Merck & Co and firstly approved for the treatment of metastatic malignant melanoma. This is the first approved therapy against PD-1.[A7624] It was approved firstly by the FDA on September 4, 2014.[L2954] Its approval in melanoma was extended to several countries such as Australia, Israel, Korea, Macau, the European Union and the United Arab Emirates.[A33350] On June 12, 2018, Pembrolizumab was approved for the treatment of cervical cancer under the status of accelerated approval.[L2955]
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 [L2727]. The U.S. Food and Drug Administration approved [DB08912](Tafilnar) and Mekinist (trametinib), administered together, for the treatment of anaplastic thyroid cancer (ATC) that cannot be removed by surgery or has spread to other parts of the body (metastatic), and has a type of abnormal gene, BRAF V600E (BRAF V600E mutation-positive) [L2726]. Thyroid cancer is a disease in which cancer cells form in the tissues of the thyroid. Anaplastic thyroid cancer is a rare, aggressive type of thyroid cancer. The National Institutes of Health (NIH) estimates there will be 53,990 new cases of thyroid cancer and an estimated 2,060 deaths from the disease in the United States in 2018. Anaplastic thyroid cancer accounts for approximately 1 to 2 percent of all thyroid cancers [L2726].
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]
DB00570VinblastineAntitumor alkaloid isolated from Vinca rosea. (Merck, 11th ed.)
DrugDrug NameTargetType
DB00041AldesleukinInterleukin-2 receptor subunit betatarget
DB00041AldesleukinInterleukin-2 receptor subunit alphatarget
DB00041AldesleukinCytokine receptor common subunit gammatarget
DB00041AldesleukinProstaglandin G/H synthase 2enzyme
DB00041AldesleukinCytosolic phospholipase A2enzyme
DB00041AldesleukinCytochrome P450 3A4enzyme
DB00041AldesleukinXanthine dehydrogenase/oxidaseenzyme
DB00041AldesleukinCytochrome P450 2E1enzyme
DB11967BinimetinibTumor necrosis factortarget
DB11967BinimetinibInterleukin-1 betatarget
DB11967BinimetinibUDP-glucuronosyltransferase 1-1enzyme
DB11967BinimetinibCytochrome P450 1A2enzyme
DB11967BinimetinibCytochrome P450 2C19enzyme
DB11967BinimetinibMitogen-activated protein kinase kinase kinase 1target
DB11967BinimetinibDual specificity mitogen-activated protein kinase kinase 2target
DB00515CisplatinCanalicular multispecific organic anion transporter 2transporter
DB00515CisplatinMultidrug resistance-associated protein 5transporter
DB00515CisplatinCanalicular multispecific organic anion transporter 1transporter
DB00515CisplatinSolute carrier family 22 member 2transporter
DB00515CisplatinHigh affinity copper uptake protein 1transporter
DB00515CisplatinProbable low affinity copper uptake protein 2transporter
DB00515CisplatinMultidrug resistance-associated protein 6transporter
DB00515CisplatinMultidrug resistance protein 1transporter
DB00515CisplatinCopper-transporting ATPase 2transporter
DB00515CisplatinCopper-transporting ATPase 1transporter
DB00515CisplatinProstaglandin G/H synthase 2enzyme
DB00515CisplatinXanthine dehydrogenase/oxidaseenzyme
DB00515CisplatinArylamine N-acetyltransferaseenzyme
DB00515CisplatinCytochrome P450 2C9enzyme
DB00515CisplatinCytochrome P450 2B6enzyme
DB00515CisplatinCytochrome P450 4A11enzyme
DB00515CisplatinATP-binding cassette sub-family G member 2transporter
DB00515CisplatinGlutathione S-transferase theta-1enzyme
DB00515CisplatinSuperoxide dismutase [Cu-Zn]enzyme
DB00515CisplatinGlutathione S-transferase Penzyme
DB00515CisplatinNAD(P)H dehydrogenase [quinone] 1enzyme
DB00515CisplatinGlutathione S-transferase Mu 1enzyme
DB00515CisplatinDNA-3-methyladenine glycosylasetarget
DB00515CisplatinSerum albumincarrier
DB00515CisplatinCopper transport protein ATOX1target
DB05239CobimetinibDual specificity mitogen-activated protein kinase kinase 1target
DB05239CobimetinibCytochrome P450 3A4enzyme
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
DB08912DabrafenibCytochrome P450 2B6enzyme
DB08912DabrafenibCytochrome P450 2C9enzyme
DB00851DacarbazineDNA polymerase alpha subunit Btarget
DB00851DacarbazineCytochrome P450 1A1enzyme
DB00851DacarbazineCytochrome P450 1A2enzyme
DB00851DacarbazineCytochrome P450 2E1enzyme
DB00851Dacarbazine6-phosphogluconate dehydrogenase, decarboxylatingtarget
DB11718EncorafenibCytochrome P450 3A4enzyme
DB11718EncorafenibCytochrome P450 2C19enzyme
DB11718EncorafenibCytochrome P450 2D6enzyme
DB11718EncorafenibSerine/threonine-protein kinase B-raftarget
DB11718EncorafenibG1/S-specific cyclin-D1target
DB00619ImatinibPlatelet-derived growth factor receptor betatarget
DB00619ImatinibTyrosine-protein kinase ABL1target
DB00619ImatinibMast/stem cell growth factor receptor Kittarget
DB00619ImatinibRET proto-oncogenetarget
DB00619ImatinibHigh affinity nerve growth factor receptortarget
DB00619ImatinibMacrophage colony-stimulating factor 1 receptortarget
DB00619ImatinibPlatelet-derived growth factor receptor alphatarget
DB00619ImatinibEpithelial discoidin domain-containing receptor 1target
DB00619ImatinibCytochrome P450 3A4enzyme
DB00619ImatinibBCR/ABL fusion protein isoform X9target
DB00619ImatinibCytochrome P450 1A2enzyme
DB00619ImatinibCytochrome P450 2D6enzyme
DB00619ImatinibCytochrome P450 2C9enzyme
DB00619ImatinibCytochrome P450 2C19enzyme
DB00619ImatinibCytochrome P450 3A5enzyme
DB00619ImatinibCytochrome P450 3A7enzyme
DB00619ImatinibSolute carrier family 22 member 1transporter
DB00619ImatinibMultidrug resistance protein 1transporter
DB00619ImatinibSolute carrier family 22 member 2transporter
DB00619ImatinibATP-binding cassette sub-family G member 2transporter
DB00619ImatinibATP-binding cassette sub-family A member 3transporter
DB00619ImatinibProstaglandin G/H synthase 1enzyme
DB00619ImatinibSerum albumincarrier
DB00619ImatinibAlpha-1-acid glycoprotein 1carrier
DB00619ImatinibBile salt export pumptransporter
DB00619ImatinibCytochrome P450 2C8enzyme
DB06186IpilimumabCytotoxic T-lymphocyte protein 4target
DB09035NivolumabProgrammed cell death protein 1target
DB01229PaclitaxelApoptosis regulator Bcl-2target
DB01229PaclitaxelTubulin beta-1 chaintarget
DB01229PaclitaxelCytochrome P450 2C8enzyme
DB01229PaclitaxelCytochrome P450 3A4enzyme
DB01229PaclitaxelCytochrome P450 3A5enzyme
DB01229PaclitaxelCytochrome P450 3A7enzyme
DB01229PaclitaxelBile salt export pumptransporter
DB01229PaclitaxelMultidrug resistance protein 1transporter
DB01229PaclitaxelMultidrug resistance-associated protein 1transporter
DB01229PaclitaxelMultidrug resistance-associated protein 7transporter
DB01229PaclitaxelCytochrome P450 19A1enzyme
DB01229PaclitaxelCytochrome P450 1B1enzyme
DB01229PaclitaxelSolute carrier organic anion transporter family member 1B3transporter
DB01229PaclitaxelNuclear receptor subfamily 1 group I member 2target
DB01229PaclitaxelMicrotubule-associated protein 4target
DB01229PaclitaxelMicrotubule-associated protein 2target
DB01229PaclitaxelMicrotubule-associated protein tautarget
DB01229PaclitaxelATP-binding cassette sub-family G member 2transporter
DB01229PaclitaxelCanalicular multispecific organic anion transporter 1transporter
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
DB08881VemurafenibCytochrome P450 2C9enzyme
DB08881VemurafenibCytochrome P450 2C8enzyme
DB08881VemurafenibCytochrome P450 2B6enzyme
DB00570VinblastineTubulin beta chaintarget
DB00570VinblastineTranscription factor AP-1target
DB00570VinblastineCytochrome P450 3A4enzyme
DB00570VinblastineMultidrug resistance protein 1transporter
DB00570VinblastineMultidrug resistance-associated protein 1transporter
DB00570VinblastineCanalicular multispecific organic anion transporter 1transporter
DB00570VinblastineMultidrug resistance-associated protein 6transporter
DB00570VinblastineBile salt export pumptransporter
DB00570VinblastineTubulin alpha-1A chaintarget
DB00570VinblastineTubulin delta chaintarget
DB00570VinblastineTubulin epsilon chaintarget
DB00570VinblastineTubulin gamma-1 chaintarget
DB00570VinblastineCytochrome P450 2D6enzyme
DB00570VinblastineSolute carrier organic anion transporter family member 1B1transporter
DrugDrug NamePhaseStatusCount
DB12768BCG vaccine1Terminated1
DB00531Cyclophosphamide1Not Yet Recruiting1
DB08912Dabrafenib1Active Not Recruiting1
DB01099Flucytosine1Active Not Recruiting1
DB06186Ipilimumab1Active Not Recruiting2
DB06132Nivolumab1Active Not Recruiting1
DB09035Nivolumab1Active Not Recruiting3
DB09037Pembrolizumab1Not Yet Recruiting1
DB08911Trametinib1Active Not Recruiting1
DB11771Tremelimumab1Active Not Recruiting1
DB00041Aldesleukin1 / 2Active Not Recruiting1
DB00041Aldesleukin1 / 2Completed2
DB00041Aldesleukin1 / 2Terminated1
DB01169Arsenic trioxide1 / 2Terminated1
DB00112Bevacizumab1 / 2Completed1
DB00112Bevacizumab1 / 2Withdrawn1
DB00515Cisplatin1 / 2Completed2
DB00531Cyclophosphamide1 / 2Active Not Recruiting2
DB00531Cyclophosphamide1 / 2Completed1
DB00531Cyclophosphamide1 / 2Terminated3
DB08912Dabrafenib1 / 2Recruiting2
DB00851Dacarbazine1 / 2Completed1
DB01254Dasatinib1 / 2Completed1
DB01262Decitabine1 / 2Completed1
DB00822Disulfiram1 / 2Terminated1
DB01073Fludarabine1 / 2Active Not Recruiting2
DB01073Fludarabine1 / 2Completed1
DB01073Fludarabine1 / 2Terminated3
DB05217GMX17771 / 2Terminated1
DB11795GSK-26367711 / 2Recruiting1
DB05996Glembatumumab vedotin1 / 2Withdrawn1
DB12827Indoximod1 / 2Active Not Recruiting1
DB06186Ipilimumab1 / 2Active Not Recruiting2
DB06186Ipilimumab1 / 2Completed1
DB06186Ipilimumab1 / 2Recruiting3
DB06186Ipilimumab1 / 2Terminated1
DB06186Ipilimumab1 / 2Withdrawn3
DB12340Navitoclax1 / 2Recruiting1
DB09035Nivolumab1 / 2Active Not Recruiting1
DB09035Nivolumab1 / 2Recruiting3
DB09035Nivolumab1 / 2Withdrawn1
DB12191Obatoclax1 / 2Terminated1
DB06603Panobinostat1 / 2Completed1
DB00022Peginterferon alfa-2b1 / 2Active Not Recruiting1
DB09037Pembrolizumab1 / 2Active Not Recruiting1
DB09037Pembrolizumab1 / 2Not Yet Recruiting1
DB09037Pembrolizumab1 / 2Recruiting3
DB00020Sargramostim1 / 2Recruiting1
DB00853Temozolomide1 / 2Completed4
DB00853Temozolomide1 / 2Terminated1
DB00853Temozolomide1 / 2Withdrawn1
DB08911Trametinib1 / 2Recruiting2
DB08881Vemurafenib1 / 2Active Not Recruiting1
DB05585Verubulin1 / 2Completed1
DB00570Vinblastine1 / 2Completed1
DB00041Aldesleukin2Active Not Recruiting3
DB11595Atezolizumab2Not Yet Recruiting1
DB00112Bevacizumab2Active Not Recruiting1
DB05239Cobimetinib2Active Not Recruiting1
DB05239Cobimetinib2Not Yet Recruiting1
DB00531Cyclophosphamide2Active Not Recruiting2
DB00531Cyclophosphamide2Not Yet Recruiting1
DB00851Dacarbazine2Active Not Recruiting1
DB01254Dasatinib2Active Not Recruiting1
DB06091Evofosfamide2Active Not Recruiting1
DB01073Fludarabine2Active Not Recruiting2
DB01073Fludarabine2Not Yet Recruiting1
DB09053Ibrutinib2Active Not Recruiting2
DB00034Interferon Alfa-2a, Recombinant2Completed1
DB00105Interferon alfa-2b2Completed1
DB06186Ipilimumab2Active Not Recruiting4
DB06186Ipilimumab2Not Yet Recruiting1
DB09035Nivolumab2Active Not Recruiting1
DB09035Nivolumab2Not Yet Recruiting1
DB01229Paclitaxel2Active Not Recruiting1
DB01229Paclitaxel2Unknown Status1
DB00073Rituximab2Unknown Status1
DB00020Sargramostim2Active Not Recruiting1
DB08881Vemurafenib2Active Not Recruiting2
DB08881Vemurafenib2Not Yet Recruiting1
DB00515Cisplatin4Unknown Status1
DB00851Dacarbazine4Unknown Status1
DB00309Vindesine4Unknown Status1
DB00041AldesleukinNot AvailableActive Not Recruiting2
DB00112BevacizumabNot AvailableNot Yet Recruiting1
DB00531CyclophosphamideNot AvailableActive Not Recruiting2
DB00927FamotidineNot AvailableActive Not Recruiting1
DB01073FludarabineNot AvailableActive Not Recruiting1
DB06186IpilimumabNot AvailableActive Not Recruiting1
DB01042MelphalanNot AvailableRecruiting1
DB09037PembrolizumabNot AvailableRecruiting1
DB12978PexidartinibNot AvailableActive Not Recruiting1