Ripretinib: First Approval

Sohita Dhillon, Sohita Dhillon

Abstract

Ripretinib (QINLOCK™) is a novel type II tyrosine switch control inhibitor being developed by Deciphera Pharmaceuticals for the treatment of KIT proto-oncogene receptor tyrosine kinase (KIT)-driven and/or platelet derived growth factor receptor A (PDGFRA)-driven cancers, including gastrointestinal stromal tumour (GIST). Ripretinib inhibits KIT and PDGFRA kinase, including wild-type, primary and secondary mutations, as well as other kinases, such as PDGFRB, TIE2, VEGFR2 and BRAF. In May 2020, oral ripretinib received its first approval in the USA for the treatment of adult patients with advanced GIST who have received prior treatment with ≥ 3 kinase inhibitors, including imatinib. The US FDA, Health Canada and the Australian Therapeutic Goods Administration collaborated on the review of the ripretinib new drug application in this indication as part of Project Orbis; regulatory review in Australia and Canada is ongoing. Clinical development for GIST, solid tumours and systemic mastocytosis is underway in several countries worldwide. This article summarizes the milestones in the development of ripretinib leading to this first approval for the treatment of advanced GIST.

Conflict of interest statement

During the peer review process the manufacturer of the agent under review was offered an opportunity to comment on the article. Changes resulting from any comments received were made by the authors on the basis of scientific completeness and accuracy. Sohita Dhillon is a contracted employee of Adis International Ltd/Springer Nature, is responsible for the article content and declares no relevant conflicts of interest.

Figures

https://www.ncbi.nlm.nih.gov/pmc/articles/instance/7595980/bin/40265_2020_1348_Figa_HTML.jpg
Key milestones in the development of ripretinib, focusing on its use in the treatment of gastrointestinal stromal tumour. GIST gastrointestinal stromal tumour, NDA New Drug Application, NDS New Drug Submission, MAA Marketing Authorisation Application, PDUFA Prescription Drug User Fee Act, RTOR Real-Time Oncology Review
https://www.ncbi.nlm.nih.gov/pmc/articles/instance/7595980/bin/40265_2020_1348_Figb_HTML.jpg
Chemical structure of ripretinib

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Source: PubMed

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