Cobimetinib (Cotellic)

General information

Class/mechanism: Tyrosine kinase inhibitor, MEK1 (mitogen-activated extracellular signal regulated kinase 1) and MEK2 inhibitor. Cobimetinib inhibits the mitogen-activated protein kinase (MAPK)/extracellular signal-related kinase (ERK) pathway by inhibiting MEK1 and MEK2. Cancers with BRAF V600E and K mutations have constitutive activation of the BRAF pathway, which includes MEK1 and MEK2. Inhibiting MEK1 and MEK2 results in inhibition of ERK and cellular proliferation.
Route: PO
Extravasation: n/a

For conciseness and simplicity, HemOnc.org currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias or the prescribing information.

Diseases for which it is used

• BRAF-mutated melanoma
• Craniopharyngioma
• Erdheim-Chester disease
• Langerhans cell histiocytosis
• Rosai-Dorfman-Destombes disease

Patient drug information

• Cobimetinib (Cotellic) package insert

History of changes in FDA indication

• 2015-11-10: Approved for the treatment of patients with unresectable or metastatic melanoma with a BRAF V600E or V600K mutation, in combination with vemurafenib. (Based on coBRIM)
• 2022-11-01: Approved for the treatment of adult patients with the family of blood diseases known as histiocytic neoplasms. These diseases include Erdheim-Chester disease, Rosai-Dorfman disease, and Langerhans cell histiocytosis. (Based on MSK 15-216)

History of changes in EMA indication

• 2015-11-20: Initial authorization in combination with vemurafenib for the treatment of patients with unresectable or metastatic melanoma with a BRAF V600 mutation.

History of changes in Health Canada indication

• 2016-02-22: Initial notice of compliance

Also Known As

• Code names: GDC-0973, XL-518
• Brand name: Cotellic