Drug intelligence / Profile preview

cetirizine + loperamide

Development stage
Unknown
Lead developer
Maryam Lustberg
Modality
Small Molecules
Administration
Oral
01

Overview

The combination of cetirizine and loperamide is a prophylactic regimen being investigated to mitigate the specific toxicities associated with AKT inhibitors, such as capivasertib. In the SAFE-CAP Phase II clinical trial led by Maryam Lustberg, this combination is administered to patients with hormone receptor-positive (HR+), HER2-negative metastatic breast cancer who are receiving capivasertib and fulvestrant. Cetirizine, a second-generation H1-antihistamine, is utilized to prevent or reduce the severity of treatment-induced skin rash, while loperamide, a mu-opioid receptor agonist, is used to manage or prevent treatment-induced diarrhea. Both rash and diarrhea are frequent and often dose-limiting adverse events of AKT inhibition therapy.

Brand names
ZyrtecImodium
Other names
cetirizine and loperamideloperamide and cetirizine
02

Targets

HRH1 (Histamine H1 Receptor)SCN5A (Sodium channel protein type 5 subunit alpha)KCNH2 (Voltage-gated potassium channel subfamily H member 2)MOR (Mu opioid receptor)CACNA1C (Voltage-dependent L-type calcium channel subunit alpha-1C)

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