Cobimetinib - CAS 934660-93-2
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Not Intended for Therapeutic Use. For research use only.
cobimetinib, also known as GDC-0973 and XL-518, is an orally bioavailable small-molecule inhibitor of mitogen-activated protein kinase kinase 1 (MAP2K1 or MEK1), with potential antineoplastic activity. MEK inhibitor GDC-0973 specifically binds to and inhibits the catalytic activity of MEK1, resulting in inhibition of extracellular signal-related kinase 2 (ERK2) phosphorylation and activation and decreased tumor cell proliferation. Preclinical studies have demonstrated that this agent is effective in inhibiting the growth of tumor cells bearing a B-RAF mutation, which has been found to be associated with many tumor types. A threonine-tyrosine kinase and a key component of the RAS/RAF/MEK/ERK signaling pathway that is frequently activated in human tumors, MEK1 is required for the transmission of growth-promoting signals from numerous receptor tyrosine kinases.
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1369665-02-0 (fumarate)
white solid powder
(S)-(3,4-difluoro-2-((2-fluoro-4-iodophenyl)amino)phenyl)(3-hydroxy-3-(piperidin-2-yl)cyclobutyl)methanone; XL518; XL 518; XL-518; GDC0973; GDC 0973; GDC-0973; cobimetinib
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1.Absorption, metabolism and excretion of cobimetinib, an oral MEK inhibitor, in rats and dogs.
Takahashi RH1, Ma S1, Yue Q1, Kim-Kang H2, Yi Y2, Ly J1, Boggs JW1, Fettes A3, McClory A4, Deng Y1, Hop CE1, Khojasteh SC1, Choo EF1. Xenobiotica. 2016 Apr 8:1-16. [Epub ahead of print]
1. The absorption, metabolism and excretion of cobimetinib, an allosteric inhibitor of MEK1/2, was characterized in mass balance studies following single oral administration of radiolabeled (14C) cobimetinib to Sprague-Dawley rats (30 mg/kg) and Beagle dogs (5 mg/kg). 2. The oral dose of cobimetinib was well absorbed (81% and 71% in rats and dogs, respectively). The maximal plasma concentrations for cobimetinib and total radioactivity were reached at 2-3 h post-dose. Drug-derived radioactivity was fully recovered (∼90% of the administered dose) with the majority eliminated in feces via biliary excretion (78% of the dose for rats and 65% for dogs). The recoveries were nearly complete after the first 48 h following dosing. 3. The metabolic profiles indicated extensive metabolism of cobimetinib prior to its elimination. For rats, the predominant metabolic pathway was hydroxylation at the aromatic core. Lower exposures for cobimetinib and total radioactivity were observed in male rats compared with female rats, which was consistent to in vitro higher clearance of cobimetinib for male rats.
2.Risk of selected dermatological toxicities in cancer patients treated with MEK inhibitors: a comparative systematic review and meta-analysis.
Abdel-Rahman O1, ElHalawani H1, Ahmed H2. Future Oncol. 2015;11(24):3307-19. doi: 10.2217/fon.15.265. Epub 2015 Nov 12.
BACKGROUND: This meta-analysis was conducted aiming at assessing the risk of selected dermatological toxicities associated with MEK inhibitors.
3.Cobimetinib Plus Vemurafenib: A Review in BRAF (V600) Mutation-Positive Unresectable or Metastatic Melanoma.
Keating GM1. Drugs. 2016 Apr;76(5):605-15. doi: 10.1007/s40265-016-0562-7.
The MEK inhibitor cobimetinib (Cotellic(®)) is indicated for the treatment of patients with BRAF (V600) mutation-positive unresectable or metastatic melanoma, in combination with the BRAF inhibitor vemurafenib (Zelboraf(®)). In the pivotal coBRIM trial, previously untreated patients with BRAF (V600) mutation-positive unresectable, stage IIIC or stage IV melanoma received cobimetinib 60 mg once daily for the first 21 days of each 28-day cycle plus vemurafenib 960 mg twice daily or vemurafenib alone. Compared with vemurafenib alone, cobimetinib plus vemurafenib significantly prolonged progression-free survival (primary endpoint) and was associated with a significantly higher overall response rate and significantly prolonged overall survival. Cobimetinib plus vemurafenib had a manageable tolerability profile. In conclusion, cobimetinib plus vemurafenib is a valuable option for use in BRAF (V600) mutation-positive unresectable or metastatic melanoma.
4.The relative clinical efficacy of trametinib-dabrafenib and cobimetinib-vemurafenib in advanced melanoma: an indirect comparison.
Galván-Banqueri M1, Ubago-Pérez R1, Molina-López T1. J Clin Pharm Ther. 2016 Apr 15. doi: 10.1111/jcpt.12390. [Epub ahead of print]
WHAT IS KNOWN AND OBJECTIVE: Melanoma causes the majority of skin cancer-related deaths. The outcome of melanoma depends on its stage at diagnosis. Currently, for patients with advanced melanoma, two MEK inhibitors (trametinib and cobimetinib) have been authorized by the European Medicines Agency. The main objective of this study was to compare the relative efficacy of trametinib-dabrafenib and cobimetinib-vemurafenib in patients with advanced melanoma through adjusted indirect treatment comparisons (ITCs).
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CAS 934660-93-2 Cobimetinib

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