Mitiperstat Explained

Legal Status:Investigational
Cas Number:1933460-19-5
Pubchem:121362450
Unii:S6GYK3X4QQ
Chemspiderid:114711423
Chembl:5095218
Stdinchi:1S/C15H15ClN4OS/c1-8(17)11-6-10(16)3-2-9(11)7-20-12-4-5-18-13(12)14(21)19-15(20)22/h2-6,8,18H,7,17H2,1H3,(H,19,21,22)/t8-/m1/s1
Stdinchikey:BHKKSKOHRFHHIN-MRVPVSSYSA-N
Smiles:C[C@H](C1=C(C=CC(=C1)Cl)CN2C3=C(C(=O)NC2=S)NC=C3)N
Iupac Name:1-2-[(1''R'')-1-Aminoethyl]-4-chlorophenylmethyl]-2-sulfanylidene-5H-pyrrolo[3,2-''d'']pyrimidin-4-one
C:15
H:15
Cl:1
N:4
O:1
S:1

Mitiperstat (AZD4831) is an irreversible inhibitor of myeloperoxidase and experimental drug in development for heart failure with preserved ejection fraction.[1] [2] [3] [4] [5] [6] [7] It is being developed by AstraZeneca.[8]

Notes and References

  1. Michaëlsson . Erik . Lund . Lars H. . Hage . Camilla . Shah . Sanjiv J. . Voors . Adriaan A. . Saraste . Antti . Redfors . Björn . Grove . Erik L. . Barasa . Anders . Richards . A. Mark . Svedlund . Sara . Lagerström-Fermér . Maria . Gabrielsen . Anders . Garkaviy . Pavlo . Gan . Li-Ming . Lam . Carolyn S.P. . Myeloperoxidase Inhibition Reverses Biomarker Profiles Associated With Clinical Outcomes in HFpEF . JACC: Heart Failure . July 2023 . 11 . 7 . 775–787 . 10.1016/j.jchf.2023.03.002. 37140510 . 258485391 . free .
  2. Lam . Carolyn S.P. . Lund . Lars H. . Shah . Sanjiv J. . Voors . Adriaan A. . Erlinge . David . Saraste . Antti . Pirazzi . Carlo . Grove . Erik L. . Barasa . Anders . Schou . Morten . Aziz . Ahmed . Svedlund . Sara . Wijngaarden . Jan Van . Lindstedt . Eva-Lotte . Gustavsson . Andreas . Nelander . Karin . Garkaviy . Pavlo . Gan . Li-Ming . Gabrielsen . Anders . Myeloperoxidase Inhibition in Heart Failure With Preserved or Mildly Reduced Ejection Fraction: SATELLITE Trial Results . Journal of Cardiac Failure . April 2023 . 10.1016/j.cardfail.2023.04.003. 37072105 . 258184680 . free .
  3. Bhattacharya . Chandrali . Sandinge . Ann-Sofie . Bragg . Ryan A. . Heijer . Maria . Yan . Jingjing . Andersson . Linda C. . Jurva . Ulrik . Pelay-Gimeno . Marta . Vaes . Wouter H.J. . de Ligt . Rianne A.F. . Gränfors . Malin . Amilon . Carl . Lindstedt . Eva-Lotte . Menakuru . Somasekhara R. . Garkaviy . Pavlo . Weidolf . Lars . Gopaul . V. Sashi . Application of Accelerator Mass Spectrometry to Characterize the Mass Balance Recovery and Disposition of AZD4831, a Novel Myeloperoxidase Inhibitor, following Administration of an Oral Radiolabeled Microtracer Dose in Humans . Drug Metabolism and Disposition . April 2023 . 51 . 4 . 451–463 . 10.1124/dmd.122.001100. 36639243 . 255800825 . free .
  4. Jurva . Ulrik . Weidolf . Lars . Sandinge . Ann-Sofie . Leandersson . Carina . Ekdahl . Anja . Li . Xue-Qing . Antonsson . Thomas . Sundell . Johan . Westerlund . Kristina . Amilon . Carl . Inghardt . Tord . Gopaul . V. Sashi . Biotransformation of the Novel Myeloperoxidase Inhibitor AZD4831 in Preclinical Species and Humans . Drug Metabolism and Disposition . April 2023 . 51 . 4 . 464–479 . 10.1124/dmd.122.001099. 36653117 . 255972963 . free . 11022936 .
  5. Nelander . Karin . Lagerstrom‐Fermer . Maria . Amilon . Carl . Michaëlsson . Erik . Heijer . Maria . Kjaer . Magnus . Russell . Muir . Han . David . Lindstedt . Eva‐Lotte . Whatling . Carl . Gan . Li‐Ming . Ericsson . Hans . Early Clinical Experience With AZD4831, A Novel Myeloperoxidase Inhibitor, Developed for Patients With Heart Failure With Preserved Ejection Fraction . Clinical and Translational Science . May 2021 . 14 . 3 . 812–819 . 10.1111/cts.12859. 32770730 . 8212712 .
  6. Gan . Li‐Ming . Lagerström‐Fermér . Maria . Ericsson . Hans . Nelander . Karin . Lindstedt . Eva‐Lotte . Michaëlsson . Erik . Kjaer . Magnus . Heijer . Maria . Whatling . Carl . Fuhr . Rainard . Safety, tolerability, pharmacokinetics and effect on serum uric acid of the myeloperoxidase inhibitor AZD4831 in a randomized, placebo‐controlled, phase I study in healthy volunteers . British Journal of Clinical Pharmacology . April 2019 . 85 . 4 . 762–770 . 10.1111/bcp.13855. 30618054 . 6422671 .
  7. Inghardt . Tord . Antonsson . Thomas . Ericsson . Cecilia . Hovdal . Daniel . Johannesson . Petra . Johansson . Carina . Jurva . Ulrik . Kajanus . Johan . Kull . Bengt . Michaëlsson . Erik . Pettersen . Anna . Sjögren . Tove . Sörensen . Henrik . Westerlund . Kristina . Lindstedt . Eva-Lotte . Discovery of AZD4831, a Mechanism-Based Irreversible Inhibitor of Myeloperoxidase, As a Potential Treatment for Heart Failure with Preserved Ejection Fraction . Journal of Medicinal Chemistry . 8 September 2022 . 65 . 17 . 11485–11496 . 10.1021/acs.jmedchem.1c02141. 36005476 . 9469207 .
  8. Web site: AstraZeneca's investigational MPO inhibitor AZD4831 shows promise in patients with heart failure and a preserved ejection fraction . AstraZeneca . 11 November 2023 . July 2021.

This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Mitiperstat".

Except where otherwise indicated, Everything.Explained.Today is © Copyright 2009-2024, A B Cryer, All Rights Reserved. Cookie policy.