Welcome to “A to Z: Drugs in Highlight
This series is designed to delve into the intricate realm of pharmaceutical drugs. As the world of pharmaceuticals continues to evolve with new discoveries and emerging challenges, we aim to shed light on the diverse array of medications available today, ranging from blockbuster medications to those that may not be as familiar. Whether you’re a healthcare professional, a student, or simply someone with a curious mind, “A to Z: Drugs in Highlight” promises to be an enlightening and engaging series.
Z is for ZELBORAF®
ZELBORAF® (from Roche and Daiichi Sankyo) is used to treat patients with melanoma (a type of skin cancer).
How it works:
ZELBORAF® is used to treat adults with melanoma that has spread or cannot be surgically removed, and only in those whose melanoma tumour cells have a specific mutation called BRAF V600.
The active substance in ZELBORAF® is vemurafenib.
Vemurafenib is an inhibitor of BRAF (a protein involved in stimulating cell division), specifically targeting the mutated form known as BRAF V600E. This mutation leads to continuous activation of the MAPK pathway, which promotes uncontrolled cell division and contributes to the development of melanoma. By selectively inhibiting BRAF V600E, vemurafenib reduces signalling through the MAPK pathway. This inhibition results in the slowing down of tumour growth and spread of the cancer cells.
ZELBORAF® is available as tablets (240 mg). The recommended dose is 960 mg (four tablets) twice daily.
Market impact:
ZELBORAF® is approved for marketing in the United States (approved by the FDA in August 2011) and in Europe (approved by the EMA in February 2012).
ZELBORAF® was co-developed by Roche and Plexxikon Inc. (which was acquired by Daiichi Sankyo Co.).
Patent protection:
There are patent rights protecting various aspects of ZELBORAF® in the United States and Europe. For example, in Europe, EP1893612 relates to a compound having the structure of Formula IIIm:
wherein R81, R83 and R112 are defined broadly. EP1893612 is due to expire in 2026. Supplementary Protection Certificates (SPCs) based on EP1893612 extend protection for “Vemurafenib and pharmaceutically acceptable salts” until February 2027.
EP2462116 relates to a process for the manufacture of the compound of formula (1),
characterized in that the compound of formula (5)
is reacted in the presence of 4-Chlorophenylboronic acid and a Palladium Catalyst to give the compound of formula (6)
and the 2,6-Dichlorbenzamide group in said compound (6) is cleaved to give the compound of formula (1).
In the United States, Novartis agreed to pay USD 182 million to settle a patent dispute with Daiichi Sankyo. The dispute centred around Novartis’ cancer drug, TAFINLAR®, which Daiichi Sankyo claimed infringed US patents 9469640 and 9844539. TAFINLAR® was acquired from GSK after a 2015 asset swap. Daiichi Sankyo alleged that GSK scientists only gathered the knowledge necessary to develop the rival drug after consulting with Plexxikon during partnership discussion that ultimately did not materialize. This settlement concluded a long-running legal battle between the two companies dating back to 2017.
Patent support from Secerna
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