molecules of the month


peripherally-restricted D2/D3 antagonist

oral agent for gastroparesis in Ph. II

up to 100 mg PO BID

JPET, Clinical Pharmacology

Altos Therapeutics / Takeda, Cambridge

Chemical structure of TAK-906 Altos Therapeutics/Takeda D2/D3 receptor antagonist
2 mins read

The Altos Therapeutics/Takeda D2/D3 receptor antagonist, TAK-906, is a peripherally-restricted, non-BBB penetrant molecule, targeting the stomach and vomiting center in the area postrema to treat gastroparesis. Gastroparesis is a chronic condition characterized by delayed gastric emptying, resulting in nausea, vomiting, pain, and anorexia. Cisapride was used off-label in the past (but was famously withdrawn due to cardiac side effects). Metoclopramide, a dopamine receptor antagonist, is approved for short term use (up to 12 weeks) and up to 5 days by the EMA, due to the increased risk of tardive dyskinesia. Peripheral restriction was employed due to known CNS side effects of D2/D3 antagonism (e.g., tardive dyskinesia). It is a great example of a peripherally-restricted drug targeting a former CNS target in a new indication.…

request a trial

You don’t have time to read everything, but you can’t afford to fall behind.

Drug Hunter Premium is drug discovery, distilled, so you can quickly catch up and make informed decisions based on industry examples.

Get ahead now by requesting a trial.

already a member? log in: