binimetinib

Binimetinib (MEK162; ARRY-438162) is a potent, adenosine triphosphate-uncompetitive, highly selective allosteric inhibitor of MEK1/2 with demonstrated on-target activity in vitro and in vivo, including models of cancer [...] In vivo, binimetinib displays broad anti-tumour activity in xenograft models derived from melanoma, colorectal cancer, non-small cell lung cancer (NSCLC), fibrosarcoma, cholangiocarcinoma, and pancreatic cancer. These non-clinical data support the use of binimetinib in a wide variety of tumour types, with a priority in tumours with aberrantly activated MAPK pathway signalling.

2017 February 28, Johanna C. Bendell et al., “A Phase 1 Dose-escalation and Expansion Study of Binimetinib (MEK162), a Potent and Selective Oral MEK1/2 Inhibitor”, in British Journal of Cancer, volume 116, Edinburgh: Nature Research, →DOI, →ISSN, →OCLC, page 576, column 1

Under development are binimetinib, a MEK inhibitor being studied in patients with NRAS-mutant melanoma, and encorafinib, a BRAF inhibitor being used in combination with binimetinib for patients with BRAF-mutant melanoma.

2018, Laurence Brunton, Bjorn Knollman, Randa Hilal-Dandan, Goodman and Gilman’s The Pharmacological Basis of Therapeutics, 13th edition, New York, N.Y.: McGraw Hill Professional, →ISBN, page 1212

The initial report of the phase I/II combination trial of encorafenib and binimetinib reported on 9 BRAF inhibitor naive and 14 BRAF inhibitor pretreated patients with metastatic BRAF mutant melanoma across a range of doses.

2018, Shane Y. Morita et al., Textbook of General Surgical Oncology, New York, N.Y.: McGraw Hill Professional, →ISBN, page 187

Binimetinib is an oral reversible inhibitor of mitogen-activated extracellular signal-regulated kinase (MEK) 1/2. [...] Binimetinib inhibits MEK 1/2 downstream from BRAF and halts cancer cell signaling and survival. [...] Binimetinib is approved in combination with encorafenib, a BRAF inhibitor, for the treatment of unresectable or metastatic melanoma with a BRAF V600E/K mutation, as detected by an FDA-approved test.

2019 July 20, Heidi Finnes, “Binimetinib (Mektovi®)”, in Oncology Times: The Newspaper for Specialists in Cancer, volume 41, number 14, Philadelphia, Pa.: Lippincott Williams & Wilkins, →DOI, →ISSN, →OCLC, page 8

Special Considerations [...] 7. Monitor patients for an increased risk of new primary cancers, both cutaneous and non-cutaneous, while on therapy and for up to 6 months following the last dose of binimetinib. [...] 10. Baseline and periodic CPK levels while on therapy, as rhabdomyolysis has been observed with binimetinib therapy.

2020, Edward Chu; Vincent T[heodore] DeVita, Jr., “Chemotherapeutic and Biologic Drugs”, in Physicians’ Cancer Chemotherapy Drug Manual 2021, Burlington, Mass.: Jones & Bartlett Learning, →ISBN, →ISSN, page 77