Firibastat

Firibastat
Clinical data
Other names	QGC-001
Legal status
Legal status	Investigational;
Identifiers
	IUPAC name (3S,3′S)-4,4′-Disulfanediylbis(3-amino-1-butanesulfonic acid);
CAS Number	648927-86-0;
PubChem CID	24851355;
DrugBank	DB13107;
ChemSpider	30649361;
UNII	638KY4573I;
ChEMBL	ChEMBL4297511;
Chemical and physical data
Formula	C8H20N2O6S4
Molar mass	368.50 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES C(CS(=O)(=O)O)[C@@H](CSSC[C@H](CCS(=O)(=O)O)N)N;
	InChI InChI=1S/C8H20N2O6S4/c9-7(1-3-19(11,12)13)5-17-18-6-8(10)2-4-20(14,15)16/h7-8H,1-6,9-10H2,(H,11,12,13)(H,14,15,16)/t7-,8-/m0/s1; Key:HJPXZXVKLGEMGP-YUMQZZPRSA-N;

Firibastat is a prodrug of two brain aminopeptidase A inhibitors, developed to treat resistant hypertension.^[1]^[2]^[3]^[4] It failed to show efficacy in a Phase III trial.^[5]

References

^ Ojha, Utkarsh; Ruddaraju, Sanjay; Sabapathy, Navukkarasu; Ravindran, Varun; Worapongsatitaya, Pitchaya; Haq, Jeesanul; Mohammed, Raihan; Patel, Vinod (2022). "Current and Emerging Classes of Pharmacological Agents for the Management of Hypertension". American Journal of Cardiovascular Drugs. 22 (3): 271–285. doi:10.1007/s40256-021-00510-9. ISSN 1175-3277. PMC 8651502. PMID 34878631.
^ Ferdinand, Keith C.; Balavoine, Fabrice; Besse, Bruno; Black, Henry R.; Desbrandes, Stephanie; Dittrich, Howard C.; Nesbitt, Shawna D. (9 July 2019). "Efficacy and Safety of Firibastat, A First-in-Class Brain Aminopeptidase A Inhibitor, in Hypertensive Overweight Patients of Multiple Ethnic Origins: A Phase 2, Open-Label, Multicenter, Dose-Titrating Study". Circulation. 140 (2): 138–146. doi:10.1161/CIRCULATIONAHA.119.040070. ISSN 0009-7322. PMID 31014072. S2CID 129943816.
^ Hansen, Emma; Grimm, Daniela; Wehland, Markus (27 January 2022). "Current Knowledge about the New Drug Firibastat in Arterial Hypertension". International Journal of Molecular Sciences. 23 (3): 1459. doi:10.3390/ijms23031459. ISSN 1422-0067. PMC 8836050. PMID 35163378.
^ Alomar, Sara Abdulrahman; Alghabban, Sarah Ali; Alharbi, Hadeel Abdulaziz; Almoqati, Mehad Fahad; Alduraibi, Yazid; Abu-Zaid, Ahmed (5 January 2021). "Firibastat, the first-in-class brain aminopeptidase a inhibitor, in the management of hypertension: A review of clinical trials". Avicenna Journal of Medicine. 11 (1): 1–7. doi:10.4103/ajm.ajm_117_20. ISSN 2231-0770. PMC 7839263. PMID 33520782.
^ "First-in-class aminopeptidase-A inhibitor fails to reduce treatment-resistant hypertension". Scientific Sessions. 9 November 2022. Retrieved 8 November 2023.

[1] Ojha, Utkarsh; Ruddaraju, Sanjay; Sabapathy, Navukkarasu; Ravindran, Varun; Worapongsatitaya, Pitchaya; Haq, Jeesanul; Mohammed, Raihan; Patel, Vinod (2022). "Current and Emerging Classes of Pharmacological Agents for the Management of Hypertension". American Journal of Cardiovascular Drugs. 22 (3): 271–285. doi:10.1007/s40256-021-00510-9. ISSN 1175-3277. PMC 8651502. PMID 34878631.

[2] Ferdinand, Keith C.; Balavoine, Fabrice; Besse, Bruno; Black, Henry R.; Desbrandes, Stephanie; Dittrich, Howard C.; Nesbitt, Shawna D. (9 July 2019). "Efficacy and Safety of Firibastat, A First-in-Class Brain Aminopeptidase A Inhibitor, in Hypertensive Overweight Patients of Multiple Ethnic Origins: A Phase 2, Open-Label, Multicenter, Dose-Titrating Study". Circulation. 140 (2): 138–146. doi:10.1161/CIRCULATIONAHA.119.040070. ISSN 0009-7322. PMID 31014072. S2CID 129943816.

[3] Hansen, Emma; Grimm, Daniela; Wehland, Markus (27 January 2022). "Current Knowledge about the New Drug Firibastat in Arterial Hypertension". International Journal of Molecular Sciences. 23 (3): 1459. doi:10.3390/ijms23031459. ISSN 1422-0067. PMC 8836050. PMID 35163378.

[4] Alomar, Sara Abdulrahman; Alghabban, Sarah Ali; Alharbi, Hadeel Abdulaziz; Almoqati, Mehad Fahad; Alduraibi, Yazid; Abu-Zaid, Ahmed (5 January 2021). "Firibastat, the first-in-class brain aminopeptidase a inhibitor, in the management of hypertension: A review of clinical trials". Avicenna Journal of Medicine. 11 (1): 1–7. doi:10.4103/ajm.ajm_117_20. ISSN 2231-0770. PMC 7839263. PMID 33520782.

[5] "First-in-class aminopeptidase-A inhibitor fails to reduce treatment-resistant hypertension". Scientific Sessions. 9 November 2022. Retrieved 8 November 2023.

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