Ertugliflozin

Ertugliflozin
Clinical data
Trade namesSteglatro
Other namesPF-04971729, ertugliflozin l-pyroglutamic acid
AHFS/Drugs.comMonograph
License data
Pregnancy
category
Routes of
administration		By mouth
Drug classAntidiabetic agent
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability~100%
Protein binding93.6%
MetabolismUGT1A9, UGT2B7
MetabolitesGlucuronides
Elimination half-life~17 hours
Excretion41% faeces, 50% urine
Identifiers
  • (1S,2S,3S,4R,5S)-5-[4-Chloro-3-(4-ethoxybenzyl)phenyl]-1-(hydroxymethyl)-6,8-dioxabicyclo[3.2.1]octane-2,3,4-triol
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
CompTox Dashboard (EPA)
ECHA InfoCard100.237.989 Edit this at Wikidata
Chemical and physical data
FormulaC22H25ClO7
Molar mass436.89 g·mol−1
3D model (JSmol)
  • CCOc1ccc(cc1)Cc2cc(ccc2Cl)[C@@]34[C@@H]([C@H]([C@@H]([C@@](O3)(CO4)CO)O)O)O
  • InChI=1S/C22H25ClO7/c1-2-28-16-6-3-13(4-7-16)9-14-10-15(5-8-17(14)23)22-20(27)18(25)19(26)21(11-24,30-22)12-29-22/h3-8,10,18-20,24-27H,2,9,11-12H2,1H3/t18-,19-,20+,21-,22-/m0/s1
  • Key:MCIACXAZCBVDEE-CUUWFGFTSA-N

Ertugliflozin, sold under the brand name Steglatro, is a medication for the treatment of type 2 diabetes.[3][4]

The most common side effects include fungal infections of the vagina and other infections of the female reproductive system.[4]

Ertugliflozin is a sodium/glucose cotransporter 2 (SGLT2) inhibitor[3][4] and is in the class of drugs known as gliflozins.[5]

In the United States, it was approved by the Food and Drug Administration for use as a monotherapy and as a fixed dose combination with either sitagliptin or with metformin.[6] In the European Union, it was approved in March 2018, for use as a monotherapy or combination therapy.[7] In September 2020, The New England Journal of Medicine reported that ertugliflozin was shown to be essentially non-inferior to placebo with respect to cardiovascular events.[8]

A combination with metformin is marketed as Segluromet and a combination with sitagliptin is marketed as Steglujan.[1][9][10][11][12]

  1. ^ a b Australian Public Assessment Report for Ertugliflozin, Ertugliflozin / Sitagliptin, Ertugliflozin / Metformin (PDF) (Report).
  2. ^ "Drug and medical device highlights 2018: Helping you maintain and improve your health". Health Canada. 14 October 2020. Retrieved 17 April 2024.
  3. ^ a b c "Steglatro- ertugliflozin tablet, film coated". DailyMed. 30 January 2020. Retrieved 24 September 2020.
  4. ^ a b c d "Steglatro EPAR". European Medicines Agency (EMA). 17 September 2018. Retrieved 24 September 2020. Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
  5. ^ Trum M, Wagner S, Maier LS, Mustroph J (June 2020). "CaMKII and GLUT1 in heart failure and the role of gliflozins". Biochimica et Biophysica Acta (BBA) - Molecular Basis of Disease. 1866 (6): 165729. doi:10.1016/j.bbadis.2020.165729. PMID 32068116. S2CID 211159566.
  6. ^ "FDA Approves SGLT2 Inhibitor Ertugliflozin for Type 2 Diabetes". MedScape.
  7. ^ "Steglatro: EPAR – Product Information" (PDF). European Medicines Agency. 4 June 2018. Archived from the original (PDF) on 18 June 2018. Retrieved 18 June 2018.
  8. ^ Cannon CP, Pratley R, Dagogo-Jack S, Mancuso J, Huyck S, Masiukiewicz U, et al. (October 2020). "Cardiovascular Outcomes with Ertugliflozin in Type 2 Diabetes". The New England Journal of Medicine. 383 (15): 1425–1435. doi:10.1056/NEJMoa2004967. PMID 32966714.
  9. ^ "Segluromet- ertugliflozin and metformin hydrochloride tablet, film coated". DailyMed. 11 August 2020. Retrieved 24 September 2020.
  10. ^ "Segluromet EPAR". European Medicines Agency (EMA). 17 September 2018. Retrieved 24 September 2020.
  11. ^ "Steglujan- ertugliflozin and sitagliptin tablet, film coated". DailyMed. U.S. National Library of Medicine. 31 January 2020. Retrieved 24 September 2020.
  12. ^ "Steglujan EPAR". European Medicines Agency (EMA). 17 September 2018. Retrieved 24 September 2020.