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Mobocertinib

Mobocertinib structure

CAS No:
1847461-43-1
Formula:
C32H39N7O4
Chemical Name:
Mobocertinib
Synonyms:
AP32788, MOBOCERTINIB;Mobocertinib;5-Pyrimidinecarboxylic acid, 2-[[4-[[2-(dimethylamino)ethyl]methylamino]-2-methoxy-5-[(1-oxo-2-propen-1-yl)amino]phenyl]amino]-4-(1-methyl-1H-indol-3-yl)-, 1-methylethyl ester;Mobocertinib (TAK788);Isopropyl 2-((5-acrylamido-4-((2-(dimethylamino)ethyl)(methyl)amino)-2-methoxyphenyl)amino)-4-(1-methyl-1H-indol-3-yl)pyrimidine-5-carboxylate;Mobocertinib (TAK788, AP32788);propan-2-yl 2-[4-[2-(dimethylamino)ethyl-methylamino]-2-methoxy-5-(prop-2-enoylamino)anilino]-4-(1-methylindol-3-yl)pyrimidine-5-carboxylate;2H6]-Mobocertinib
Categories:
Pharmaceutical Intermediates > Bulk Drug Intermediates

Description

Mobocertinib is under investigation in clinical trial NCT04129502 (TAK-788 as First-line Treatment Versus Platinum-based Chemotherapy for Non-small Cell Lung Cancer (NSCLC) With EGFR Exon 20 Insertion Mutations).|Mobocertinib is an orally available inhibitor of human epidermal growth factor receptor (EGFR) exon 20 insertion mutations, with antineoplastic activity. Upon oral administration, mobocertinib, and its active metabolites, specifically and irreversibly binds to and inhibits exon 20 insertion mutations of EGFR. This prevents EGFR-mediated signaling and leads to cell death in tumor cells expressing exon 20 insertion mutations. In addition, mobocertinib may inhibit the activity of other EGFR family members, such as human epidermal growth factor receptor 2 (HER2; ERBB2) and HER4. EGFR, HER-2 and -4 are receptor tyrosine kinases often mutated in numerous tumor cell types. They play key roles in tumor cell proliferation and tumor vascularization.

Mobocertinib is derived from osimertinib, a second-generation TKI which exhibits only limited activity against several resistant EGFRex20ins mutants. Both inhibitors are structurally identical except that the pyrimidine ring of moboceritinib incorporates a snugly fitting isopropyl ester group that targets a previously unoccupied pocket, resulting in expanded coverage of EGFRex20ins mutations as well as improved selectivity over wildtype EGFR vs. osimertinib.

Class: receptor tyrosine kinaseTreatment: NSCLC with EGFR alterationsOral bioavailability = 37%Elimination half-life = 18 h

Mobocertinib Basic Attributes

Molecular Weight：

585.71

Exact Mass：

585.30635275

UNII：

39HBQ4A67L

NCI Thesaurus Code：

C126752

Color/Form：

Off-white to light yellow

Characteristics

Critical Temperature & Pressure：

Store at -20°C

Mobocertinib Use and Manufacturing

Mobocertinib (TAK-788) is an orally active and irreversible EGFR/HER2 inhibitor. Mobocertinib effectively inhibits oncogenic variants containing mutations that activate the EGFRex20ins, with selectivity superior to that of wild-type EGFR. Mobocertinib is FDA-approved for the treatment of patients with non-small cell lung cancer (NSCLC) who have a HER2 mutation or an EGFR mutation, including an exon 20 insertion mutation. Mobocertinib is approved by the FDA for the treatment of patients with non-small cell lung cancer (NSCLC) who have HER2 mutations or EGFR mutations, including exon 20 insertion mutations.

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