Drug intelligence / Profile preview

darapladib + diltiazem

Development stage
Phase 1
Lead developer
GSK
Modality
Small Molecules
Administration
Oral
01

Overview

Darapladib + diltiazem is an unbranded combination of two small-molecule pharmaceuticals: darapladib and diltiazem. - Darapladib is a selective inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2), an enzyme implicated in the inflammatory processes of atherosclerosis. It was developed primarily for reducing cardiovascular events in patients with coronary heart disease, though its clinical development was discontinued after failing to achieve efficacy endpoints in late-phase trials. - Diltiazem is a benzothiazepine calcium channel blocker (CCB) widely used to treat hypertension, angina pectoris, and certain arrhythmias. It acts by inhibiting the influx of calcium ions into cardiac and smooth muscle cells, resulting in vasodilation, decreased heart rate, and reduced cardiac workload. There are no approved formulations marketed as a fixed combination of darapladib and diltiazem. Their combination is not standard therapy and, if used together, is off-label or investigational. No unique pharmacologic synergy or adverse interactions are specifically documented for this particular combination; however, both can affect cardiovascular parameters and their concurrent use should be monitored for additive effects on heart rate, blood pressure, and potential pharmacokinetic interactions due to metabolism via cytochrome P450 enzymes.

02

Targets

PLA2G7 (Platelet-activating factor acetylhydrolase)CACNA1S (Voltage-dependent L-type calcium channel subunit alpha-1S)CACNA1C (Voltage-dependent L-type calcium channel subunit alpha-1C)

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