General Information of Drug (ID: DMYP4XC)

Drug Name
Norgestimate Drug Info
Synonyms
Norgestimato; Norgestimatum; Dexnorgestrel acetime; Norgestrel oxime acetate; D 138; ORF 10131; RWJ 10131; Norgestimato [INN-Spanish]; Norgestimatum [INN-Latin]; ORF-10131; Ortho-Prefest; RWJ-10131; Norgestimate (USP/INN); Norgestimate [USAN:INN:BAN]; D-13beta-Ethyl-17alpha-ethynyl-17beta-acetoxygon-4-en-3-oneoxime; D-13-beta-Ethyl-17-alpha-ethynyl-17-beta-acetoxygon-4-en-3-one oxime; [(3E,8R,9S,10R,13S,14S,17R)-13-ethyl-17-ethynyl-3-hydroxyimino-1,2,6,7,8,9,10,11,12,14,15,16-dodecahydrocyclopenta[a]phenanthren-17-yl] acetate; (+)-13-Ethyl-17-hydroxy-18,19-dinor-17alpha-pregn-4-en-20-yn-3-one oxime acetate (ester); (17-alpha)-17-(Acetyloxy)-13-ethyl-18,19-dinorpregn-4-en-20-yn-3-one 3-oxime; (17alpha)-17-(Acetyloxy)-13-ethyl-18,19-dinorpregn-4-en-20-yn-3-one 3-oxime; (3E)-17alpha-ethynyl-3-(hydroxyimino)-18a-homoestr-4-en-17beta-yl acetate
Indication
Disease Entry ICD 11 Status REF
Acne vulgaris ED80 Approved [1]
Contraception QA21 Approved [2]
Hot flushes GA30 Approved [1]
Obsolete atrophic vulva Approved [1]
Therapeutic Class
Contraceptive Agents
Cross-matching ID
PubChem CID
6540478
ChEBI ID
CHEBI:50815
CAS Number
CAS 20799-27-3
TTD Drug ID
DMYP4XC
INTEDE Drug ID
DR1178

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Progesterone receptor (PGR) TTUV8G9 PRGR_HUMAN Agonist [3]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID Highest Status REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Approved [4]

The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
Progesterone receptor (PGR) DTT PGR 1.848 1.888 1.263 0.138
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 11.692 6.58 4.984 9.089
Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

The Studied Disease Acne vulgaris
ICD Disease Classification ED80
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Progesterone receptor (PGR) DTT PGR 3.26E-38 -3.79 -2.5
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 2.20E-02 -1.08E-01 -2.31E-01
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1 Norgestimate FDA Label
2 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7091).
3 Pharmacological profile of progestins. Maturitas. 2008 Sep-Oct;61(1-2):151-7.
4 Metabolite identification, reaction phenotyping, and retrospective drug-drug interaction predictions of 17-deacetylnorgestimate, the active component of the oral contraceptive norgestimate. Drug Metab Dispos. 2017 Jun;45(6):676-685.