Olmutinib (

INN Inns are generally establishments or buildings where travelers can seek lodging, and usually, food and drink. Inns are typically located in the country or along a highway. Before the advent of motorized transportation, they also provided accomm ...

) is an investigational anti-cancer drug. It acts by covalently bonding to a cysteine residue near the kinase domain of

epidermal growth factor receptor The epidermal growth factor receptor (EGFR; ErbB-1; HER1 in humans) is a transmembrane protein that is a receptor (biochemistry), receptor for members of the epidermal growth factor family (EGF family) of extracellular protein ligand (biochemistry ...

(EGFR). In the US, it was given a

breakthrough therapy Breakthrough therapy is a United States Food and Drug Administration designation that expedites drug development that was created by Congress under Section 902 of the 9 July 2012 Food and Drug Administration Safety and Innovation Act. The FDA's "b ...

designation in

non-small cell lung cancer Non-small-cell lung cancer (NSCLC), or non-small-cell lung carcinoma, is any type of epithelial lung cancer other than small-cell lung cancer (SCLC). NSCLC accounts for about 85% of all lung cancers. As a class, NSCLCs are relatively insensitiv ...

(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 T790M, also known as Thr790Met, is a gatekeeper mutation of the epidermal growth factor receptor (EGFR). The mutation substitutes a threonine (T) with a methionine (M) at position 790 of exon 20, affecting the ATP binding pocket of the EGFR kinas ...

mutation of EGFR. Resistance to olmutinib has been reported; a person's cancer started progressing after they developed a C797S mutation in EGFR. Olmutinib was discovered by Hanmi Pharmaceutical and licensed to

Boehringer Ingelheim C.H. Boehringer Sohn AG & Co. is the parent company of the Boehringer Ingelheim group, which was founded in 1885 by Albert Boehringer (1861–1939) in Ingelheim am Rhein, Germany. As of 2018, Boehringer Ingelheim is one of the world's List of la ...

in 2015 in an agreement with a $50 million up front payment and up $680 million in milestones. In November 2015 Hanmi granted an exclusive license to sell olmutinib in China to the Chinese company ZAI Labs. On September 30, 2016, Korean regulatory authorities issued a safety alert about olmutinib in which it described two cases of

toxic epidermal necrolysis Toxic epidermal necrolysis (TEN), also known as Lyell's syndrome, is a type of severe skin reaction. Together with Stevens–Johnson syndrome (SJS) it forms a spectrum of disease, with TEN being more severe. Early symptoms include fever and f ...

, one of which was fatal, and a case of

Stevens–Johnson syndrome Stevens–Johnson syndrome (SJS) is a type of severe skin reaction. Together with toxic epidermal necrolysis (TEN) and #Classification, Stevens–Johnson/toxic epidermal necrolysis (SJS/TEN) overlap, they are considered febrile mucocutaneous d ...

; 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.

References

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