Description
Cotellic (Cobimetinib) 20mg Online
Cotellic (Cobimetinib) is an anticancer drug used to treat inoperable or metastatic melanoma with a BRAF V600 mutation in adult patients in combination with vemurafenib. Cotellic is a kinase inhibitor indicated for the treatment of patients with BRAF V600E or BRAF V600K mutation-positive advanced melanoma, in combination with vemurafenib. Cotellic selectively blocks the activity of MEK, a cellular protein that is part of the mitogen-activated protein kinase (MAPK) signalling pathway, an important cascade of signalling proteins in cells that regulates cellular growth and survival.
Following cutaneous malignancies or premalignant conditions occurred in the Cotellic with vemurafenib arm and the vemurafenib arm, respectively: cutaneous squamous cell carcinoma (cuSCC) or keratoacanthoma (KA) (6% and 20%), basal cell carcinoma (4.5% and 2.4%), and second primary melanoma (0.8% and 2.4%). Among patients receiving Cotellic with vemurafenib, the median time to detection of first cuSCC/KA was 4 months (range: 2 to 11 months), and the median time to detection of basal cell carcinoma was 4 months (range: 27 days to 13 months). The time to onset in the two patients with second primary melanoma was 9 months and 12 months.
Perform dermatologic evaluations prior to initiation of therapy and every 2 months while on therapy. Manage suspicious skin lesions with excision and dermatopathologic evaluation. No dose modifications are recommended for Cotellic [see Dosage and Administration (2.3)]. Conduct dermatologic monitoring for 6 months following discontinuation of Cotellic when administered with vemurafenib.
In biochemical and structural studies, the interaction of cobimetinib with MEK was shown, with little sensitivity to the dynamic conformational changes observed during the transition of MEK to the phosphorylated form. As a result, cobimetinib retains binding ability and inhibitory activity during MEK phosphorylation. Cobimetinib showed the highest activity against tumor cell lines and tumors with high levels of MEK phosphorylation, which is often observed in tumors with BRAF mutations.
