Temanogrel

Temanogrel

Clinical data
Other names	APD-791; APD791
Routes of administration	Oral[1]
Drug class	Serotonin 5-HT2A receptor antagonist
Identifiers
IUPAC name 3-methoxy-N-[3-(2-methylpyrazol-3-yl)-4-(2-morpholin-4-ylethoxy)phenyl]benzamide
CAS Number	887936-68-7
PubChem CID	11604525
ChemSpider	9779281
UNII	F42Z27575A
KEGG	D09976
ChEBI	CHEBI:177604
ChEMBL	ChEMBL1084617
Chemical and physical data
Formula	C24H28N4O4
Molar mass	436.512 g·mol^−1
3D model (JSmol)	Interactive image
SMILES CN1C(=CC=N1)C2=C(C=CC(=C2)NC(=O)C3=CC(=CC=C3)OC)OCCN4CCOCC4
InChI InChI=1S/C24H28N4O4/c1-27-22(8-9-25-27)21-17-19(26-24(29)18-4-3-5-20(16-18)30-2)6-7-23(21)32-15-12-28-10-13-31-14-11-28/h3-9,16-17H,10-15H2,1-2H3,(H,26,29) Key:ZEOQUKRCASTCFR-UHFFFAOYSA-N

Temanogrel (INNTooltip International Nonproprietary Name, USANTooltip United States Adopted Name; developmental code name APD791) is a serotonin 5-HT_2A receptor antagonist and inverse agonist which is under development for the treatment of myocardial ischemia and Raynaud's disease.^[1][2] It was also being developed for arterial thrombosis and acute coronary syndromes, but development for the former use was suspended and development for the latter indication was discontinued.^[1] The drug is taken orally.^[1] Temanogrel is highly selective for the serotonin 5-HT_2A receptor, with more than 2,000-fold selectivity for this receptor over the serotonin 5-HT_2B and 5-HT_2C receptors and lack of activity at a variety of other G protein-coupled receptors (GPCRs).^[3][4] As of September 2022, it is in phase 2 clinical trials for myocardial ischemia and Raynaud's disease.^[1]

See also

• Serotonin 5-HT_2A receptor antagonist

References

1. "Temanogrel". AdisInsight. 20 September 2022. Retrieved 16 January 2026.
2. Alenazy FO, Thomas MR (January 2021). "Novel antiplatelet targets in the treatment of acute coronary syndromes". Platelets. 32 (1): 15–28. doi:10.1080/09537104.2020.1763731. PMID 32529932. APD791 is a high-affinity, selective 5-HT2A antagonist that improves coronary patency during recurrent thrombosis in preclinical models [83,84]. A phase I study for APD791 was initiated to assess its pharmacokinetics, pharmacodynamics and safety upon co-administration with aspirin and clopidogrel in healthy subjects planned in South Korea. However, the Clinicaltrials.gov record indicated that the trial was terminated on the basis of the sponsor's decision (Clinicaltrials.gov identifier NCT02419820) in 2019 [85].
3. Adams JW, Ramirez J, Shi Y, Thomsen W, Frazer J, Morgan M, Edwards JE, Chen W, Teegarden BR, Xiong Y, Al-Shamma H, Behan DP, Connolly DT (October 2009). "APD791, 3-methoxy-n-(3-(1-methyl-1h-pyrazol-5-yl)-4-(2-morpholinoethoxy)phenyl)benzamide, a novel 5-hydroxytryptamine 2A receptor antagonist: pharmacological profile, pharmacokinetics, platelet activity and vascular biology". J Pharmacol Exp Ther. 331 (1): 96–103. doi:10.1124/jpet.109.153189. PMID 19628629.
4. Xiong Y, Teegarden BR, Choi JS, Strah-Pleynet S, Decaire M, Jayakumar H, Dosa PI, Casper MD, Pham L, Feichtinger K, Ullman B, Adams J, Yuskin D, Frazer J, Morgan M, Sadeque A, Chen W, Webb RR, Connolly DT, Semple G, Al-Shamma H (June 2010). "Discovery and structure-activity relationship of 3-methoxy-N-(3-(1-methyl-1H-pyrazol-5-yl)-4-(2-morpholinoethoxy)phenyl)benzamide (APD791): a highly selective 5-hydroxytryptamine2A receptor inverse agonist for the treatment of arterial thrombosis". J Med Chem. 53 (11): 4412–4421. doi:10.1021/jm100044a. PMID 20455563.