The patent application WO2003077914A1, filed in 2003 and published in 2003, relates to binimetinib [1]. This application is available on Google Patents [1]. Binimetinib is a MEK inhibitor used in cancer treatment [2].
What is Binimetinib?
Binimetinib is an oral selective inhibitor of MEK1 and MEK2 [2]. These enzymes are part of the RAS/RAF/MEK/ERK pathway, which is frequently activated in various cancers [2]. By inhibiting MEK, binimetinib can block downstream signaling that promotes cell proliferation and survival [2].
When does the patent for Binimetinib expire?
Patent expiry dates are complex and can vary based on different patents covering the compound, its manufacturing process, and its uses. For binimetinib, the primary composition of matter patents are likely to have expired or be nearing expiration in various regions. For example, U.S. Patent No. 8,005,770, which covers binimetinib, had an original expiry in 2026 but may be subject to patent term extensions [3]. Specific expiry timelines can be tracked on resources like DrugPatentWatch.com [4].
What other patents are related to Binimetinib?
Beyond the composition of matter patent, other patents may cover specific formulations, manufacturing processes, or therapeutic uses of binimetinib. Patent applications such as WO2003077914A1 represent early filings in the development of the drug [1]. Companies often file multiple patents throughout a drug's lifecycle to protect different aspects of their intellectual property [4].
How is Binimetinib used in cancer treatment?
Binimetinib is approved for the treatment of unresectable or metastatic melanoma with a BRAF V600E or V600K mutation, in combination with encorafenib [5]. It is also investigated for other BRAF-mutated cancers [2].
What are the side effects of Binimetinib?
Common side effects associated with binimetinib therapy include fatigue, nausea, diarrhea, vomiting, abdominal pain, and rash [5]. More serious side effects can include heart problems, eye disorders, and liver issues [5].
What companies are involved with Binimetinib?
Binimetinib was developed by Array BioPharma, which was acquired by Pfizer in 2019 [6]. It is marketed by Pfizer under the brand names Mektovi®, often in combination with encorafenib (Braftovi®) [5].
How does Binimetinib compare to other MEK inhibitors?
Other MEK inhibitors, such as trametinib and cobimetinib, are also used in cancer therapy, often in combination with BRAF inhibitors [7]. These drugs target the same pathway but may have differences in their potency, selectivity, pharmacokinetic profiles, and side effect profiles [7].
What is the mechanism of action for Binimetinib?
Binimetinib selectively inhibits MEK1 and MEK2. MEK proteins are kinases that lie downstream of BRAF in the MAPK signaling pathway. Activation of this pathway leads to cell proliferation, survival, and differentiation [2]. In cancers with mutations in BRAF, this pathway is constitutively active, driving tumor growth [2].
What is the regulatory status of Binimetinib?
Binimetinib has received regulatory approval from agencies like the U.S. Food and Drug Administration (FDA) and the European Medicines Agency (EMA) for specific indications, notably in combination with encorafenib for melanoma [5].
Sources:
[1] Google Patents (WO2003077914A1)
[2] ClinicalTrials.gov (Binimetinib)
[3] U.S. Patent 8,005,770
[4] DrugPatentWatch.com
[5] Mektovi® (binimetinib) Prescribing Information
[6] Pfizer Inc. Acquisition of Array BioPharma Inc.
[7] National Cancer Institute (MEK Inhibitors)