General Information of Drug (ID: DME7VZD)

Drug Name
Vilaprisan Drug Info
Synonyms
Vilaprisan; UNII-IN59K53GI9; BAY1002670; IN59K53GI9; 1262108-14-4; Vilaprisan [INN]; BAY 1002670; Vilaprisan [USAN:INN]; Vilaprisan (USAN/INN); SCHEMBL2121854; CHEMBL3989936; BCP24069; DB11971; 20,20,21,21,21-Pentafluoro-17-hydroxy-11beta-(4-(methanesulfonyl)phenyl)-19-nor-17alpha-pregna-4,9-dien-3-one; 19-Norpregna-4,9-dien-3-one, 20,20,21,21,21-pentafluoro-17-hydroxy-11-(4-(methylsulfonyl)phenyl)-, (11beta,17alpha)-
Indication
Disease Entry ICD 11 Status REF
Endometriosis GA10 Phase 2 [1]
Cross-matching ID
PubChem CID
50915138
CAS Number
CAS 1262108-14-4
TTD Drug ID
DME7VZD
INTEDE Drug ID
DR1831

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DME
Drug Status:
Approved Drug(s)
Drug(s) Targeting Progesterone receptor (PGR)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Progesterone DMUY35B Amenorrhea GA20.0 Approved [4]
Desogestrel DM27U4Y Contraception QA21 Approved [5]
Ulipristal DMBNI20 Contraception QA21 Approved [6]
Etonogestrel DMKA8J4 Contraception QA21 Approved [7]
Megestrol DMDH9KX Breast cancer 2C60-2C65 Approved [8]
Segesterone acetate; ethinyl estradiol DMFEGB0 Contraception QA21 Approved [9]
Norgestimate DMYP4XC Acne vulgaris ED80 Approved [7]
Dydrogesterone DMAKIDV Menstrual disorder GA20.3 Approved [10]
Medroxyprogesterone DMBGWPH Solid tumour/cancer 2A00-2F9Z Approved [10]
Ethynodiol Diacetate DMZM84R Contraception QA21 Approved [11]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Metabolized By Cytochrome P450 3A4 (CYP3A4)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [12]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [13]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [14]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [15]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [16]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [17]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [18]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [19]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [13]
Verapamil DMA7PEW Angina pectoris BA40 Approved [20]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [21]

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Progesterone receptor (PGR) TTUV8G9 PRGR_HUMAN Antagonist [2]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Substrate [3]
Succinic semialdehyde reductase (AKR7A2) DE4G629 ARK72_HUMAN Substrate [3]

References

1 ClinicalTrials.gov (NCT02465814) Assess Safety and Efficacy of Vilaprisan in Patients With Uterine Fibroids.
2 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800033939)
3 Characterization of the pharmacokinetics of vilaprisan: bioavailability, excretion, biotransformation, and drug-drug interaction potential. Clin Pharmacokinet. 2018 Aug;57(8):1001-1015.
4 Clinical pipeline report, company report or official report of lipocine.
5 Preclinical experience with two selective progesterone receptor modulators on breast and endometrium. Steroids. 2000 Oct-Nov;65(10-11):733-40.
6 Mullard A: 2010 FDA drug approvals. Nat Rev Drug Discov. 2011 Feb;10(2):82-5.
7 Pharmacological profile of progestins. Maturitas. 2008 Sep-Oct;61(1-2):151-7.
8 Focus on anastrozole and breast cancer. Curr Med Res Opin. 2003;19(8):683-8.
9 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89.
10 Dienogest is a selective progesterone receptor agonist in transactivation analysis with potent oral endometrial activity due to its efficient pharm... Steroids. 2008 Feb;73(2):222-31.
11 Contribution of functional groups of 19-nor-progestogens to binding to progesterone and estradiol-17beta receptors in rabbit uterus. Endocrinology. 1977 Jun;100(6):1579-84.
12 Expression levels and activation of a PXR variant are directly related to drug resistance in osteosarcoma cell lines. Cancer. 2007 Mar 1;109(5):957-65.
13 Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
14 Comprehensive evaluation of tamoxifen sequential biotransformation by the human cytochrome P450 system in vitro: prominent roles for CYP3A and CYP2D6. J Pharmacol Exp Ther. 2004 Sep;310(3):1062-75.
15 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
16 Metabolic interactions between acetaminophen (paracetamol) and two flavonoids, luteolin and quercetin, through in-vitro inhibition studies. J Pharm Pharmacol. 2017 Dec;69(12):1762-1772.
17 Potent mechanism-based inhibition of CYP3A4 by imatinib explains its liability to interact with CYP3A4 substrates. Br J Pharmacol. 2012 Apr;165(8):2787-98.
18 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
19 The metabolism of zidovudine by human liver microsomes in vitro: formation of 3'-amino-3'-deoxythymidine. Biochem Pharmacol. 1994 Jul 19;48(2):267-76.
20 Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.
21 Naturally occurring variants of human aldo-keto reductases with reduced in vitro metabolism of daunorubicin and doxorubicin. J Pharmacol Exp Ther. 2010 Dec;335(3):533-45.