Drug intelligence / Profile preview

abemaciclib + loperamide

Development stage
Unknown
Lead developer
Eli Lilly
Modality
Small Molecules
Administration
Oral
01

Overview

Abemaciclib + loperamide is a **non-fixed combination therapy** used specifically for the management of abemaciclib-induced diarrhea in breast cancer patients. **Abemaciclib** is an orally administered selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), which blocks cell cycle progression in hormone receptor-positive, HER2-negative breast cancer. **Loperamide** is an antidiarrheal agent that acts on the mu-opioid receptors in the gut to decrease gastrointestinal motility and fluid secretion, providing symptomatic relief of diarrhea. This combination is not a single pharmaceutical formulation but reflects the clinical practice of prescribing loperamide to manage a common and often dose-limiting adverse effect of abemaciclib therapy[1][2][4]. The combination is primarily intended for use in breast cancer patients receiving abemaciclib, where loperamide is started at the first sign of loose stools to allow continuation of cancer therapy and to maintain quality of life[1].

Other names
abemaciclib plus loperamideabemaciclib and loperamide
02

Targets

DOR (Opioid Receptor Delta 1)CDK6 (Cyclin-dependent kinase 6)CDK4 (Cyclin-dependent kinase 4)MOR (Mu opioid receptor)CDK9 (Cyclin-dependent kinase 9)GSK3 (Glycogen synthase kinase 3 beta)KOR (Kappa opioid receptor)

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