Drug intelligence / Profile preview

mobocertinib + loperamide

Development stage
Unknown
Lead developer
Takeda
Modality
Small Molecules
Administration
Oral
01

Overview

Mobocertinib + loperamide is a combination regimen used primarily in the management of non-small cell lung cancer (NSCLC) in adults with EGFR exon 20 insertion mutations. Mobocertinib is an oral, irreversible tyrosine kinase inhibitor (TKI) specifically targeting mutated forms of the epidermal growth factor receptor (EGFR). Loperamide, an opioid receptor agonist acting on the gut, is used adjunctively to manage mobocertinib-induced diarrhea due to its antimotility effects. This combination does not constitute a fixed-dose pharmaceutical product, but rather co-administration for supportive care. Mobocertinib is developed by Takeda for cancer therapy, while loperamide is a widely available antidiarrheal agent.

02

Targets

EGFR ex20ins (Epidermal growth factor receptor exon 20 mutant)MOR (Mu opioid receptor)EGFR T790M (Epidermal growth factor receptor T790M mutant)

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