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| SMILES = C(CS(=O)(=O)O)[C@@H](CSSC[C@H](CCS(=O)(=O)O)N)N
| SMILES = C(CS(=O)(=O)O)[C@@H](CSSC[C@H](CCS(=O)(=O)O)N)N
<!-- Chemical and physical data -->
<!-- Chemical and physical data -->
| IUPAC_name = (3''S'',3&prime;''S'')-4,4&prime;-Disulfanediylbis(3-amino-1-butanesulfonic acid)
| IUPAC_name = (3''S'',3{{prime}}''S'')-4,4{{prime}}-Disulfanediylbis(3-amino-1-butanesulfonic acid)
| C = 8 | H = 20 | N = 2 | O = 6 | S = 4
| C = 8 | H = 20 | N = 2 | O = 6 | S = 4
}}
}}


'''Firibastat ''' is a [[prodrug]] of two [[brain aminopeptidase A inhibitor]]s, developed to treat [[resistant hypertension]].<ref>{{cite journal |last1=Ojha |first1=Utkarsh |last2=Ruddaraju |first2=Sanjay |last3=Sabapathy |first3=Navukkarasu |last4=Ravindran |first4=Varun |last5=Worapongsatitaya |first5=Pitchaya |last6=Haq |first6=Jeesanul |last7=Mohammed |first7=Raihan |last8=Patel |first8=Vinod |title=Current and Emerging Classes of Pharmacological Agents for the Management of Hypertension |journal=American Journal of Cardiovascular Drugs |date=2022 |volume=22 |issue=3 |pages=271–285 |doi=10.1007/s40256-021-00510-9 |pmid=34878631 |pmc=8651502 |issn=1175-3277}}</ref><ref>{{cite journal |last1=Ferdinand |first1=Keith C. |last2=Balavoine |first2=Fabrice |last3=Besse |first3=Bruno |last4=Black |first4=Henry R. |last5=Desbrandes |first5=Stephanie |last6=Dittrich |first6=Howard C. |last7=Nesbitt |first7=Shawna D. |title=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 |journal=Circulation |date=9 July 2019 |volume=140 |issue=2 |pages=138–146 |doi=10.1161/CIRCULATIONAHA.119.040070 |pmid=31014072 |s2cid=129943816 |url=https://www.ahajournals.org/doi/10.1161/CIRCULATIONAHA.119.040070 |language=en |issn=0009-7322|doi-access=free }}</ref><ref>{{cite journal |last1=Hansen |first1=Emma |last2=Grimm |first2=Daniela |last3=Wehland |first3=Markus |title=Current Knowledge about the New Drug Firibastat in Arterial Hypertension |journal=International Journal of Molecular Sciences |date=27 January 2022 |volume=23 |issue=3 |pages=1459 |doi=10.3390/ijms23031459 |pmid=35163378 |pmc=8836050 |issn=1422-0067 |doi-access=free }}</ref><ref>{{cite journal |last1=Alomar |first1=Sara Abdulrahman |last2=Alghabban |first2=Sarah Ali |last3=Alharbi |first3=Hadeel Abdulaziz |last4=Almoqati |first4=Mehad Fahad |last5=Alduraibi |first5=Yazid |last6=Abu-Zaid |first6=Ahmed |title=Firibastat, the first-in-class brain aminopeptidase a inhibitor, in the management of hypertension: A review of clinical trials |journal=Avicenna Journal of Medicine |date=5 January 2021 |volume=11 |issue=1 |pages=1–7 |doi=10.4103/ajm.ajm_117_20 |pmid=33520782 |pmc=7839263 |issn=2231-0770 |doi-access=free }}</ref> It failed to show efficacy in a Phase III trial.<ref>{{cite web |title=First-in-class aminopeptidase-A inhibitor fails to reduce treatment-resistant hypertension |url=https://sessions.hub.heart.org/aha-22/article/22539144/firstinclass-aminopeptidasea-inhibitor-fails-to-reduce-treatmentresistant-hypertension |website=Scientific Sessions |access-date=8 November 2023 |language=en-us |date=9 November 2022}}</ref>
'''Firibastat ''' is a [[prodrug]] of two [[brain aminopeptidase A inhibitor]]s, developed to treat [[resistant hypertension]].<ref>{{cite journal |last1=Ojha |first1=Utkarsh |last2=Ruddaraju |first2=Sanjay |last3=Sabapathy |first3=Navukkarasu |last4=Ravindran |first4=Varun |last5=Worapongsatitaya |first5=Pitchaya |last6=Haq |first6=Jeesanul |last7=Mohammed |first7=Raihan |last8=Patel |first8=Vinod |title=Current and Emerging Classes of Pharmacological Agents for the Management of Hypertension |journal=American Journal of Cardiovascular Drugs |date=2022 |volume=22 |issue=3 |pages=271–285 |doi=10.1007/s40256-021-00510-9 |pmid=34878631 |pmc=8651502 |issn=1175-3277}}</ref><ref>{{cite journal |last1=Ferdinand |first1=Keith C. |last2=Balavoine |first2=Fabrice |last3=Besse |first3=Bruno |last4=Black |first4=Henry R. |last5=Desbrandes |first5=Stephanie |last6=Dittrich |first6=Howard C. |last7=Nesbitt |first7=Shawna D. |title=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 |journal=Circulation |date=9 July 2019 |volume=140 |issue=2 |pages=138–146 |doi=10.1161/CIRCULATIONAHA.119.040070 |pmid=31014072 |s2cid=129943816 |language=en |issn=0009-7322|doi-access=free }}</ref><ref>{{cite journal |last1=Hansen |first1=Emma |last2=Grimm |first2=Daniela |last3=Wehland |first3=Markus |title=Current Knowledge about the New Drug Firibastat in Arterial Hypertension |journal=International Journal of Molecular Sciences |date=27 January 2022 |volume=23 |issue=3 |pages=1459 |doi=10.3390/ijms23031459 |pmid=35163378 |pmc=8836050 |issn=1422-0067 |doi-access=free }}</ref><ref>{{cite journal |last1=Alomar |first1=Sara Abdulrahman |last2=Alghabban |first2=Sarah Ali |last3=Alharbi |first3=Hadeel Abdulaziz |last4=Almoqati |first4=Mehad Fahad |last5=Alduraibi |first5=Yazid |last6=Abu-Zaid |first6=Ahmed |title=Firibastat, the first-in-class brain aminopeptidase a inhibitor, in the management of hypertension: A review of clinical trials |journal=Avicenna Journal of Medicine |date=5 January 2021 |volume=11 |issue=1 |pages=1–7 |doi=10.4103/ajm.ajm_117_20 |pmid=33520782 |pmc=7839263 |issn=2231-0770 |doi-access=free }}</ref> It failed to show efficacy in a Phase III trial.<ref>{{cite web |title=First-in-class aminopeptidase-A inhibitor fails to reduce treatment-resistant hypertension |url=https://sessions.hub.heart.org/aha-22/article/22539144/firstinclass-aminopeptidasea-inhibitor-fails-to-reduce-treatmentresistant-hypertension |website=Scientific Sessions |access-date=8 November 2023 |language=en-us |date=9 November 2022}}</ref>
==References==
==References==
{{reflist}}
{{reflist}}
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[[Category:Sulfonic acids]]
[[Category:Sulfonic acids]]
[[Category:Diamines]]
[[Category:Diamines]]
[[Category:Disulfides]]
[[Category:Organic disulfides]]

Latest revision as of 21:00, 7 February 2024

Firibastat
Clinical data
Other namesQGC-001
Legal status
Legal status
  • Investigational
Identifiers
  • (3S,3′S)-4,4′-Disulfanediylbis(3-amino-1-butanesulfonic acid)
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC8H20N2O6S4
Molar mass368.50 g·mol−1
3D model (JSmol)
  • C(CS(=O)(=O)O)[C@@H](CSSC[C@H](CCS(=O)(=O)O)N)N
  • 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

[edit]
  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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