Olmutinib (
INN)[1] is an investigational anti-cancer drug. It acts by covalently bonding to a cysteine residue near the kinase domain of
epidermal growth factor receptor (EGFR).[2]
In the US, it was given a
breakthrough therapy designation in
non-small cell lung cancer (NSCLC) in December 2015, and In South Korea, the drug was approved in May 2016 for the second-line treatment of NSCLC with the
T790M mutation of EGFR.[2] Resistance to olmutinib has been reported; a person's cancer started progressing after they developed a C797S mutation in EGFR.[2][3]
Olmutinib was discovered by
Hanmi Pharmaceutical and licensed to
Boehringer Ingelheim in 2015 in an agreement with a $50 million up front payment and up $680 million in milestones.[4] In November 2015 Hanmi granted an exclusive license to sell olmutinib in China to the Chinese company ZAI Labs.[5]
On September 30, 2016, Korean regulatory authorities issued a safety alert about olmutinib in which it described two cases of
toxic epidermal necrolysis, one of which was fatal, and a case of
Stevens–Johnson syndrome; Boeheringer announced the termination its deal with Hanmi the same day, citing that the decision came after a review of "all available clinical data" on the drug, and also referring to competing drugs.[6]
References
^"Olmutinib". AdisInsight. Springer Nature Switzerland AG. Retrieved 28 February 2017.
^Passaro A, Guerini-Rocco E, Pochesci A, Vacirca D, Spitaleri G, Catania CM, et al. (March 2017). "Targeting EGFR T790M mutation in NSCLC: From biology to evaluation and treatment". Pharmacological Research. 117: 406–415.
doi:
10.1016/j.phrs.2017.01.003.
PMID28089942.
S2CID45855336.