Compounds > vilaprisan
Page last updated: 2024-11-13

vilaprisan

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

vilaprisan: a progesterone receptor modulator; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID50915138
CHEMBL ID3989936
SCHEMBL ID2121854
MeSH IDM0591891

Synonyms (31)

Synonym
SCHEMBL2121854
bay-1002670
20,20,21,21,21-pentafluoro-17-hydroxy-11beta-[4-(methanesulfonyl)phenyl]-19-nor-17alpha-pregna-4,9-dien-3-one
vilaprisan [jan]
vilaprisan [usan]
19-norpregna-4,9-dien-3-one, 20,20,21,21,21-pentafluoro-17-hydroxy-11-(4-(methylsulfonyl)phenyl)-, (11.beta.,17.alpha.)-
vilaprisan [who-dd]
vilaprisan
in59k53gi9 ,
unii-in59k53gi9
vilaprisan [inn]
vilaprisan [usan:inn]
19-norpregna-4,9-dien-3-one, 20,20,21,21,21-pentafluoro-17-hydroxy-11-(4-(methylsulfonyl)phenyl)-, (11beta,17alpha)-
bay 1002670
20,20,21,21,21-pentafluoro-17-hydroxy-11beta-(4-(methanesulfonyl)phenyl)-19-nor-17alpha-pregna-4,9-dien-3-one
1262108-14-4
bay1002670
AC-30930
DB11971
bay1002670; bay-1002670; bay 1002670; bay-10-02670; bay10-02670; bay 10-02670
BCP24069
(8s,11r,13s,14s,17r)-17-hydroxy-13-methyl-11-(4-(methylsulfonyl)phenyl)-17-(perfluoroethyl)-1,2,6,7,8,11,12,13,14,15,16,17-dodecahydro-3h-cyclopenta[a]phenanthren-3-one
CHEMBL3989936
(8s,11r,13s,14s,17s)-17-hydroxy-13-methyl-11-(4-methylsulfonylphenyl)-17-(1,1,2,2,2-pentafluoroethyl)-1,2,6,7,8,11,12,14,15,16-decahydrocyclopenta[a]phenanthren-3-one
vilaprisan (jan/usan/inn)
D11181
Q27280805
19-norpregna-4,9-dien-3-one, 20,20,21,21,21-pentafluoro-17-hydroxy-11-[4-(methylsulfonyl)phenyl]-, (11beta,17alpha)-
DTXSID201110777
jufwqqvhqfduod-anrpbidpsa-n
AKOS040754354

Research Excerpts

Overview

Vilaprisan (VPR) is a new orally available selective progesterone receptor modulator (SPRM), with anti-proliferative activity against uterine fibroids (UFs) Vilaprisa markedly reduces the growth of human leiomyoma tissue in a preclinical model of uterine Fibroids.

ExcerptReferenceRelevance
"Vilaprisan is a highly potent selective progesterone receptor modulator in development for the treatment of symptomatic uterine fibroids and endometriosis. "( Clinical Pharmacokinetics and Pharmacodynamics of the Selective Progesterone Receptor Modulator Vilaprisan: A Comprehensive Overview.
Frei, M; Höchel, J; Ploeger, BA; Rottmann, A; Schultze-Mosgau, MH, 2022)		2.38
"Vilaprisan (VPR) is a new orally available selective progesterone receptor modulator (SPRM), with anti-proliferative activity against uterine fibroids (UFs). "( Vilaprisan, a New Selective Progesterone Receptor Modulator in Uterine Fibroid Pharmacotherapy-Will it Really be a Breakthrough?
Barra, F; Caruso, S; Cianci, A; Ciebiera, M; Ferrero, S; Jakiel, G; Laganà, AS; Sierant, A; Vilos, GA; Vitale, SG, 2020)		3.44
"Vilaprisan is a novel powerful SPRM."( Vilaprisan for treating uterine fibroids.
Ajossa, S; Corda, V; Giancane, E; Mais, V; Marotto, MF; Melis, GB; Neri, M; Paoletti, AM; Pilloni, M; Piras, B; Saba, A, 2018)		2.64
"Vilaprisan (BAY 1002670) is a novel, highly potent selective progesterone receptor modulator that markedly reduces the growth of human leiomyoma tissue in a preclinical model of uterine fibroids (UFs)."( Pharmacodynamics and safety of the novel selective progesterone receptor modulator vilaprisan: a double-blind, randomized, placebo-controlled phase 1 trial in healthy women.
Bell, D; Kaiser, A; Koch, M; Rohde, B; Schultze-Mosgau, MH; Schütt, B; Seitz, C, 2016)		2.1
"Vilaprisan is a novel, potent, and highly selective progesterone receptor modulator, which might offer a promising option for the treatment of uterine fibroids."( Pharmacokinetics and safety of the selective progesterone receptor modulator vilaprisan in healthy postmenopausal women
.
Hafner, FT; Hoechel, J; Kaiser, A; Rohde, B; Schuett, B; Schultze-Mosgau, MH; Zollmann, F, 2017)		2.13

Toxicity

ExcerptReferenceRelevance
" Safety assessments included adverse events (AEs), endometrial thickness and histology, laboratory parameters, vital signs and 12-lead electrocardiography."( Pharmacodynamics and safety of the novel selective progesterone receptor modulator vilaprisan: a double-blind, randomized, placebo-controlled phase 1 trial in healthy women.
Bell, D; Kaiser, A; Koch, M; Rohde, B; Schultze-Mosgau, MH; Schütt, B; Seitz, C, 2016)		0.66
" Safety assessments included vital signs, ECGs, clinical laboratory tests, and adverse events."( Pharmacokinetics and safety of the selective progesterone receptor modulator vilaprisan in healthy postmenopausal women
.
Hafner, FT; Hoechel, J; Kaiser, A; Rohde, B; Schuett, B; Schultze-Mosgau, MH; Zollmann, F, 2017)		0.68
" Mild to moderate adverse events occurred with similar frequency at all dose levels."( Pharmacokinetics and safety of the selective progesterone receptor modulator vilaprisan in healthy postmenopausal women
.
Hafner, FT; Hoechel, J; Kaiser, A; Rohde, B; Schuett, B; Schultze-Mosgau, MH; Zollmann, F, 2017)		0.68

Pharmacokinetics

ExcerptReferenceRelevance
" Blood samples for pharmacokinetic (PK) profiles were collected over 14 days after single dose (sd) and multiple dose (md; day 28)."( Pharmacokinetics and safety of the selective progesterone receptor modulator vilaprisan in healthy postmenopausal women
.
Hafner, FT; Hoechel, J; Kaiser, A; Rohde, B; Schuett, B; Schultze-Mosgau, MH; Zollmann, F, 2017)		0.68
"In this phase 1, open-label, nonrandomised, parallel-group, pharmacokinetic study, men and women with mild or moderate hepatic impairment (Child-Pugh grade A or B) and control participants with normal hepatic function matched by age, weight and sex received a single oral 2 mg dose of vilaprisan."( Effect of hepatic impairment on the pharmacokinetics of vilaprisan: An open-label, single-dose, parallel-group study.
Chattopadhyay, N; Halabi, A; Ligges, S; Riecke, K; Schultze-Mosgau, MH; Zimmermann, T, 2019)		0.94
"The SPRM VPR interfered with the pharmacodynamic effects of the COC."( The effects of vilaprisan on the pharmacodynamics and pharmacokinetics of a combined oral contraceptive-A randomized controlled trial.
Casjens, M; Draeger, C; Loewen, S; Rohde, B; Schultze-Mosgau, MH; Schütt, B; Zimmermann, T, 2021)		0.97

Bioavailability

ExcerptReferenceRelevance
" The absolute oral bioavailability of vilaprisan was ~ 60%."( Characterization of the Pharmacokinetics of Vilaprisan: Bioavailability, Excretion, Biotransformation, and Drug-Drug Interaction Potential.
Brooks, A; Bush, J; Höchel, J; Prien, O; Rottmann, A; Schultze-Mosgau, MH; Zimmermann, T, 2018)		1.01

Dosage Studied

ExcerptRelevanceReference
" self-assessed bleeding intensity of 'none' or 'spotting') using Bayesian dose-response estimation with incorporated prior information."( Pharmacodynamics and safety of the novel selective progesterone receptor modulator vilaprisan: a double-blind, randomized, placebo-controlled phase 1 trial in healthy women.
Bell, D; Kaiser, A; Koch, M; Rohde, B; Schultze-Mosgau, MH; Schütt, B; Seitz, C, 2016)		0.66
" The primary outcome was the estimated dose-response curve of the observed non-bleeding rate during Days 10-84 of treatment, excluding the endometrial biopsy day and 2 days after biopsy."( Pharmacodynamics and safety of the novel selective progesterone receptor modulator vilaprisan: a double-blind, randomized, placebo-controlled phase 1 trial in healthy women.
Bell, D; Kaiser, A; Koch, M; Rohde, B; Schultze-Mosgau, MH; Schütt, B; Seitz, C, 2016)		0.66
"Exposure to vilaprisan increased roughly dose-proportionally in the dose range studied and accumulated after multiple dosing as expected based on t1/2, indicating linear pharmacokinetics of vilaprisan in the expected therapeutic dose range."( Pharmacokinetics and safety of the selective progesterone receptor modulator vilaprisan in healthy postmenopausal women
.
Hafner, FT; Hoechel, J; Kaiser, A; Rohde, B; Schuett, B; Schultze-Mosgau, MH; Zollmann, F, 2017)		1.06
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (19)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's13 (68.42)24.3611
2020's6 (31.58)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 31.86

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index31.86 (24.57)
Research Supply Index3.40 (2.92)
Research Growth Index4.57 (4.65)
Search Engine Demand Index36.32 (26.88)
Search Engine Supply Index1.88 (0.95)

This Compound (31.86)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials10 (52.63%)5.53%
Reviews4 (21.05%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other5 (26.32%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
ethinyl estradiol
Ethinyl Estradiol: A semisynthetic alkylated ESTRADIOL with a 17-alpha-ethinyl substitution. It has high estrogenic potency when administered orally, and is often used as the estrogenic component in ORAL CONTRACEPTIVES.. 17alpha-ethynylestradiol : A 3-hydroxy steroid that is estradiol substituted by a ethynyl group at position 17. It is a xenoestrogen synthesized from estradiol and has been shown to exhibit high estrogenic potency on oral administration.		3.71117-hydroxy steroid;
3-hydroxy steroid;
terminal acetylenic compound		xenoestrogen
mifepristone
Mifepristone: A progestational and glucocorticoid hormone antagonist. Its inhibition of progesterone induces bleeding during the luteal phase and in early pregnancy by releasing endogenous prostaglandins from the endometrium or decidua. As a glucocorticoid receptor antagonist, the drug has been used to treat hypercortisolism in patients with nonpituitary CUSHING SYNDROME.		3.27103-oxo-Delta(4) steroid;
acetylenic compound;
tertiary amino compound		abortifacient;
contraceptive drug;
hormone antagonist;
synthetic oral contraceptive
glucuronic acid
Glucuronic Acid: A sugar acid formed by the oxidation of the C-6 carbon of GLUCOSE. In addition to being a key intermediate metabolite of the uronic acid pathway, glucuronic acid also plays a role in the detoxification of certain drugs and toxins by conjugating with them to form GLUCURONIDES.. D-glucuronic acid : The D-enantiomer of glucuronic acid.. D-glucopyranuronic acid : A D-glucuronic acid in cyclic pyranose form.		2.1710D-glucuronic acidalgal metabolite
ulipristal acetate
RTI 3021-012: progesterone receptor antagonist. ulipristal acetate : A 20-oxo steroid obtained by acetylation of the 17-hydroxy group of (11beta,17alpha)-17-acetyl-11-[4-(dimethylamino)phenyl]-3-oxoestra-4,9-dien-17-ol (ulipristal). A selective progesterone receptor modulator, which is employed as an emergency contraceptive.		5.853120-oxo steroid;
3-oxo-Delta(4) steroid;
acetate ester;
steroid ester;
tertiary amino compound		contraceptive drug;
progesterone receptor modulator;
progestin
bilirubin
[no description available]		7.1710biladienes;
dicarboxylic acid		antioxidant;
human metabolite;
mouse metabolite
lonaprisan
lonaprisan: structure in first source		2.1710
asoprisnil
asoprisnil: structure in first source		3.2710
telapristone acetate
telapristone acetate: structure in first source		3.2710steroid ester
rifampin
Rifampin: A semisynthetic antibiotic produced from Streptomyces mediterranei. It has a broad antibacterial spectrum, including activity against several forms of Mycobacterium. In susceptible organisms it inhibits DNA-dependent RNA polymerase activity by forming a stable complex with the enzyme. It thus suppresses the initiation of RNA synthesis. Rifampin is bactericidal, and acts on both intracellular and extracellular organisms. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1160)		2.1710cyclic ketal;
hydrazone;
N-iminopiperazine;
N-methylpiperazine;
rifamycins;
semisynthetic derivative;
zwitterion		angiogenesis inhibitor;
antiamoebic agent;
antineoplastic agent;
antitubercular agent;
DNA synthesis inhibitor;
EC 2.7.7.6 (RNA polymerase) inhibitor;
Escherichia coli metabolite;
geroprotector;
leprostatic drug;
neuroprotective agent;
pregnane X receptor agonist;
protein synthesis inhibitor
ConditionIndicatedRelationship StrengthStudiesTrials
Liver Dysfunction
[description not available]		04.9921
Liver Diseases
Pathological processes of the LIVER.		04.9921
Fibroid
[description not available]		09.1893
Cancer of the Uterus
[description not available]		08.3452
Leiomyoma
A benign tumor derived from smooth muscle tissue, also known as a fibroid tumor. They rarely occur outside of the UTERUS and the GASTROINTESTINAL TRACT but can occur in the SKIN and SUBCUTANEOUS TISSUE, probably arising from the smooth muscle of small blood vessels in these tissues.		113.62186
Uterine Neoplasms
Tumors or cancer of the UTERUS.		08.3452
Kidney Failure
A severe irreversible decline in the ability of kidneys to remove wastes, concentrate URINE, and maintain ELECTROLYTE BALANCE; BLOOD PRESSURE; and CALCIUM metabolism.		03.6411
Renal Insufficiency
Conditions in which the KIDNEYS perform below the normal level in the ability to remove wastes, concentrate URINE, and maintain ELECTROLYTE BALANCE; BLOOD PRESSURE; and CALCIUM metabolism. Renal insufficiency can be classified by the degree of kidney damage (as measured by the level of PROTEINURIA) and reduction in GLOMERULAR FILTRATION RATE.		03.6411
Heavy Menstrual Bleeding
[description not available]		05.9722
Menorrhagia
Excessive uterine bleeding during MENSTRUATION.		05.9722
Postpartum Amenorrhea
[description not available]		03.5611
Amenorrhea
Absence of menstruation.		03.5611
Hemorrhage, Uterine
[description not available]		03.0910
Uterine Hemorrhage
Bleeding from blood vessels in the UTERUS, sometimes manifested as vaginal bleeding.		03.0910
Female Genital Diseases
[description not available]		02.5220
Genital Diseases, Female
Pathological processes involving the female reproductive tract (GENITALIA, FEMALE).		02.5220
Pregnancy
The status during which female mammals carry their developing young (EMBRYOS or FETUSES) in utero before birth, beginning from FERTILIZATION to BIRTH.		02.1710