From Wikipedia, the free encyclopedia
Chemical compound
Tanaproget (
INN; developmental code names NSP-989, WAY-166989) is an investigational
nonsteroidal
progestin.
[1] It is a high
affinity, high
efficacy, and very
selective
agonist of the
progesterone receptor (PR).
[1] Due to its much more selective binding profile relative to most conventional, steroidal progestins, tanaproget may prove to produce fewer
side effects in comparison.
[1] As of December 2010,
[2] it is in
phase II
clinical trials in the process of being developed for
clinical use as a
contraceptive by
Ligand Pharmaceuticals.
[3]
[4]
An
analog of tanaproget,
4-fluoropropyltanaproget (18F), has been developed as a
radiotracer for imaging of the PR in
positron emission tomography.
[5]
See also
References
- ^
a
b
c Zhang Z, Olland AM, Zhu Y, et al. (August 2005).
"Molecular and pharmacological properties of a potent and selective novel nonsteroidal progesterone receptor agonist tanaproget". J. Biol. Chem. 280 (31): 28468–75.
doi:
10.1074/jbc.M504144200.
PMID
15937332.
-
^
Tanaproget
-
^ Bapst JL, Ermer JC, Ferron GM, Foss D, Orczyk GP (November 2006). "Pharmacokinetics and safety of tanaproget, a nonsteroidal progesterone receptor agonist, in healthy women". Contraception. 74 (5): 414–8.
doi:
10.1016/j.contraception.2006.06.004.
PMID
17046384.
-
^ Bayés M, Rabasseda X, Prous JR (September 2005). "Gateways to clinical trials". Methods Find Exp Clin Pharmacol. 27 (7): 505–22.
PMID
16258596.
-
^ Lee JH, Zhou HB, Dence CS, Carlson KE, Welch MJ, Katzenellenbogen JA (June 2010). "Development of [F-18]fluorine-substituted Tanaproget as a progesterone receptor imaging agent for positron emission tomography". Bioconjug. Chem. 21 (6): 1096–104.
doi:
10.1021/bc1001054.
PMID
20496889.
|
---|
PRTooltip Progesterone receptor | Agonists |
- Testosterone derivatives: Progestins:
6,6-Difluoronorethisterone
-
6,6-Difluoronorethisterone acetate
-
17α-Allyl-19-nortestosterone
-
Allylestrenol
-
Altrenogest
-
Chloroethynylnorgestrel
-
Cingestol
-
Danazol
-
Desogestrel
-
Dienogest
-
Ethinylandrostenediol
-
Ethisterone
-
Ethynerone
-
Etonogestrel
-
Etynodiol
-
Etynodiol diacetate
-
Gestodene
-
Gestrinone
-
Levonorgestrel
-
Levonorgestrel esters (e.g.,
levonorgestrel butanoate)
-
Lynestrenol
-
Lynestrenol phenylpropionate
-
Metynodiol
-
Metynodiol diacetate
-
Norelgestromin
-
Norethisterone (norethindrone)
-
Norethisterone esters (e.g.,
norethisterone acetate,
norethisterone enanthate)
-
Noretynodrel
-
Norgesterone
-
Norgestimate
-
Norgestrel
-
Norgestrienone
-
Norvinisterone
-
Oxendolone
-
Quingestanol
-
Quingestanol acetate
-
Tibolone
-
Tigestol
-
Tosagestin; Anabolic–androgenic steroids:
11β-Methyl-19-nortestosterone
-
11β-Methyl-19-nortestosterone dodecylcarbonate
-
19-Nor-5-androstenediol
-
19-Nor-5-androstenedione
-
19-Nordehydroepiandrosterone
-
Bolandiol
-
Bolandiol dipropionate
-
Bolandione
-
Dimethisterone
-
Dienedione
-
Dienolone
-
Dimethandrolone
-
Dimethandrolone buciclate
-
Dimethandrolone dodecylcarbonate
-
Dimethandrolone undecanoate
-
Dimethyldienolone
-
Dimethyltrienolone
-
Ethyldienolone
-
Ethylestrenol (ethylnandrol)
-
Methyldienolone
-
Metribolone (R-1881)
-
Methoxydienone (methoxygonadiene)
-
Mibolerone
-
Nandrolone
-
Nandrolone esters (e.g.,
nandrolone decanoate,
nandrolone phenylpropionate)
-
Norethandrolone
-
Normethandrone (methylestrenolone, normethandrolone, normethisterone)
-
RU-2309
-
Tetrahydrogestrinone
-
Trenbolone (trienolone)
-
Trenbolone esters (e.g.,
trenbolone acetate,
trenbolone enanthate)
-
Trendione
-
Trestolone
-
Trestolone acetate
|
---|
Mixed (
SPRMsTooltip Selective progesterone receptor modulators) | |
---|
Antagonists | |
---|
|
---|
mPRTooltip Membrane progesterone receptor (
PAQRTooltip Progestin and adipoQ receptor) | |
---|
|