Drug intelligence / Profile preview

CP-945598 + diltiazem

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

Overview

CP-945598 + diltiazem is a combination of two investigational and marketed drugs: CP-945598, a potent and selective cannabinoid CB1 receptor antagonist developed for the treatment of metabolic diseases such as obesity, and diltiazem, a calcium channel blocker used for hypertension, angina, and certain heart rhythm disorders. CP-945598 inhibits basal and agonist-mediated CB1 receptor signaling and demonstrates dose-dependent weight loss in preclinical studies, while showing negligible affinity for the CB2 receptor. By contrast, diltiazem inhibits calcium influx into cardiac and vascular smooth muscle, leading to vasodilation, reduced cardiac workload, and decreased blood pressure. The combination is a hypothetical or experimental regimen with no marketed fixed-dose product, studied for potential additive or synergistic effects in metabolic or cardiovascular diseases.

02

Targets

CNR1 (Cannabinoid receptor 1)CACNA1C (Voltage-dependent L-type calcium channel subunit alpha-1C)

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