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sumatriptan + promethazine
- Development stage
- Phase 2
- Lead developer
- Charleston Laboratories
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
Sumatriptan + promethazine is a fixed-dose combination of two small molecule drugs developed primarily for the acute treatment of migraine and associated nausea or vomiting. Sumatriptan is a selective serotonin 5-HT₁B/₁D receptor agonist that acts as an antimigraine agent by causing cranial vasoconstriction and inhibiting pro-inflammatory neuropeptide release. Promethazine is a first-generation phenothiazine antihistamine with antiemetic, anticholinergic, and sedative properties; it works mainly as a histamine H1 receptor antagonist and muscarinic receptor antagonist to reduce nausea and vomiting. The combination aims to address both headache pain (sumatriptan) and migraine-associated gastrointestinal symptoms (promethazine). The formulation CL-H1T, developed by Charleston Laboratories, has reached phase III clinical trials for the treatment of migraine as well as prevention/treatment of nausea and vomiting[3][4][1].
- Brand names
- CL-H1TCL-H-1TCL-H 1T
- Other names
- promethazine/sumatriptansumatriptan + promethazine
02
Targets
HTR1B (5-Hydroxytryptamine Receptor 1B)HTR1D (5-hydroxytryptamine receptor 1D)mAChR (Muscarinic acetylcholine receptors)HRH1 (Histamine H1 Receptor)
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