`
`https://www.cancer.gov/publications/dictionaries/cancer-drug/def/pan-...
`
`D ) NATIONAL CANCER INSTITUTE
`pan-mutant-lDHl inhibitor BAY1436032
`An orally available pan-inhibitor of mutant forms of the metabolic enzyme isocitrate dehydrogenase type 1
`(IDH1; IDH-1; IDH1 [NADP+] soluble), including forms with mutations of arginine 132 (IDH1(R132)), with
`potential antineoplastic activity. Upon administration, pan-mutant-IDH-1 inhibitor BAY-1436032 specifically
`inhibits the activity of IDH1 mutant forms, which prevents the formation of the oncometabolite
`2-hydroxyglutarate (2HG) from alpha-ketoglutarate (a-KG). This prevents 2HG-mediated signaling and leads to
`both an induction of cellular differentiation and an inhibition of cellular proliferation in tumor cells expressing
`IDH1 mutant forms. IDH1 mutations, including IDH1(R132) mutations, are highly expressed in certain
`malignancies; they initiate and drive cancer growth by both blocking cell differentiation and catalyzing the
`formation of 2HG.
`
`Check for active clinical trials using this agent
`View this agent in the NCI Thesaurus
`
`Code name:
`
`BAY 1436032
`BAY-1436032
`BAY1436032
`
`Chemical structure:
`
`3-(2-((4-(trifluoromethoxy)phenyl)amino)-1-((1 R,SR)-3,3,5-
`trimethylcyclohexyl)-1 H-benzo[d]imidazol-5-yl)propanoic acid
`
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`1 of 1
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`8/12/2022, 7:05 AM
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`Rigel Exhibit 1042
`Page 1 of 1
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