Reaction: Ertugliflozin to 3 products

Reaction
Ertugliflozin
DB11827
Ertugliflozin M4a metabolite
DBMET01912
Ertugliflozin M4b metabolite
DBMET01911
Ertugliflozin M4c metabolite
DBMET01910
Reaction type
glucuronidation
Direction
Major circulating metabolite?
No
Spontaneous?
No
Activity
active
References
  1. Miao Z, Nucci G, Amin N, Sharma R, Mascitti V, Tugnait M, Vaz AD, Callegari E, Kalgutkar AS: Pharmacokinetics, metabolism, and excretion of the antidiabetic agent ertugliflozin (PF-04971729) in healthy male subjects. Drug Metab Dispos. 2013 Feb;41(2):445-56. doi: 10.1124/dmd.112.049551. Epub 2012 Nov 20. [Article]
  2. Lapham K, Callegari E, Cianfrogna J, Lin J, Niosi M, Orozco CC, Sharma R, Goosen TC: In Vitro Characterization of Ertugliflozin Metabolism by UDP-Glucuronosyltransferase and Cytochrome P450 Enzymes. Drug Metab Dispos. 2020 Dec;48(12):1350-1363. doi: 10.1124/dmd.120.000171. Epub 2020 Oct 5. [Article]
Comments
Not Available
Enzymes
EnzymeKmVmaxRole
UDP-glucuronosyltransferase 1-9Not AvailableNot Availableconfirmed
UDP-glucuronosyltransferase 2B7Not AvailableNot Availableconfirmed