Tosagestin

Tosagestin
Clinical data

Routes of administration	Oral
Identifiers
IUPAC name (1S,2R,10R,11S,14R,15S)-14-ethynyl-14-hydroxy-15-methyl-17-methylidenetetracyclo[8.7.0.0²,⁷.0¹¹,¹⁵]heptadeca-6,12-dien-5-one
Synonyms	Exogestin, letogestin^[1]
CAS Number	110072-15-6
PubChem (CID)	159355
ChemSpider	140146
UNII	YS7Z529O22
KEGG	D06197
ChEMBL	CHEMBL2107658
Chemical and physical data
Formula	C₂₁H₂₄O₂
Molar mass	308.41406 g/mol
3D model (Jmol)	Interactive image
SMILES CC12CC(=C)C3C(C1C=CC2(C#C)O)CCC4=CC(=O)CCC34
InChI InChI=1S/C21H24O2/c1-4-21(23)10-9-18-17-7-5-14-11-15(22)6-8-16(14)19(17)13(2)12-20(18,21)3/h1,9-11,16-19,23H,2,5-8,12H2,3H3/t16-,17-,18-,19+,20-,21-/m0/s1 Key:YJSTYQGZKJHXLN-OLGWUGKESA-N

Tosagestin (INN, USAN) (developmental code name Org 30659), also known as 11-methylene-D-15-norethisterone or 17α-hydroxy-11-methylene-19-norpregna-4,15-dien-20-yn-3-one, is a selective, steroidal progestin of the 19-nortestosterone group that was under development by Organon in the United States and Europe as a hormonal contraceptive (in combination with ethinyl estradiol) and for the treatment of menopausal symptoms but was never marketed.^[2]^[3]^[4]^[5]^[6]

References

↑ Martin Negwer; Hans-Georg Scharnow (2001). Organic-chemical drugs and their synonyms: (an international survey). Wiley-VCH. p. 2104. ISBN 978-3-527-30247-5.
↑ World Health Organization (2013), The use of stems in the selection of International Nonproprietary Names (INN) for pharmaceutical substances (PDF), p. 95
↑ AdisInsight, Tosagestin, Springer, retrieved 12 July 2016
↑ Verhoeven CH, Krebbers SF, Wagenaars GN, Booy CJ, Groothuis GM, Olinga P, Vos RM (1998). "In vitro and in vivo metabolism of the progestagen Org 30659 in several species". Drug Metab. Dispos. 26 (11): 1102–12. PMID 9806953.
↑ de Visser, S.J.; Uchida, N.; van Vliet-Daskalopoulou, E.; Fukazawa, I.; van Doorn, M.B.A.; van den Heuvel, M.W.; Machielsen, C.S.M.; Uchida, E.; Cohen, A.F. (2003). "Pharmacokinetic differences between Caucasian and Japanese subjects after single and multiple doses of a potential combined oral contraceptive (Org 30659 and EE)". Contraception. 68 (3): 195–202. doi:10.1016/S0010-7824(03)00140-9. ISSN 0010-7824. PMID 14561540.
↑ Obruca, Andreas; Korver, Tjeerd; Huber, Johannes; Killick, Stephen R; Landgren, Britt-Marie; Struijs, Martin J (2001). "Ovarian function during and after treatment with the new progestagen Org 30659". Fertility and Sterility. 76 (1): 108–115. doi:10.1016/S0015-0282(01)01824-6. ISSN 0015-0282. PMID 11438328.

External links

Tosagestin - AdisInsight

Progesterone receptor modulators

Agonists	Progesterone derivatives: 5α-Dihydroprogesterone 9α-Bromo-11-ketoprogesterone 11-Dehydroprogesterone 11-Deoxycorticosterone 16α-Hydroxyprogesterone 20α-Dihydroprogesterone Dimepregnen Diosgenin Progesterone Quingestrone Retroprogesterone derivatives: Dydrogesterone Retroprogesterone Ro 6-3129 Trengestone 17α-Substituted progesterone derivatives: 17α-Hydroxyprogesterone (hydroxyprogesterone) 17α-Methylprogesterone Acetomepregenol (mepregenol diacetate) Algestone Algestone acetonide Algestone acetophenide Anagestone Anagestone acetate Butagest (buterol) Chlormadinone Chlormadinone acetate Cismadinone Cismadinone acetate Clogestone Clogestone acetate Clomegestone Clomegestone acetate Cyproterone acetate Delmadinone Delmadinone acetate Edogestrone Flugestone Flugestone acetate Flumedroxone Flumedroxone acetate Gestaclone Haloprogesterone Hydromadinone (hydromadinone acetate) Hydroxyprogesterone acetate Hydroxyprogesterone caproate (hydroxyprogesterone hexanoate) Hydroxyprogesterone heptanoate (hydroxyprogesterone enanthate) Mecigestone (pentarane B) Medrogestone Medroxyprogesterone Medroxyprogesterone acetate Megestrol Megestrol acetate Melengestrol Melengestrol acetate Mometasone Mometasone furoate Osaterone Osaterone acetate Pentagestrone Pentagestrone acetate Pentarane A Proligestone 19-Norprogesterone derivatives: 19-Norprogesterone Amadinone Amadinone acetate Demegestone Gestadienol Gestonorone caproate (gestronol hexanoate) Gestronol (gestonorone) Nomegestrol Nomegestrol acetate Norgestomet Org-2058 Oxogestone Oxogestone phenpropionate Promegestone Segesterone Segesterone acetate (nestorone) Trimegestone Testosterone derivatives: 6,6-Difluoronorethisterone 11β-Methyl-19-nortestosterone 11β-Methyl-19-nortestosterone dodecylcarbonate 19-Nor-5-androstenediol 19-Nor-5-androstenedione Δ^4-Tibolone Allylestrenol Altrenogest Bolandiol Bolandiol dipropionate Bolandione Chloroethynyl norgestrel Cingestol Danazol Desogestrel Dienedione Dienogest Dienolone Dimethandrolone Dimethandrolone buciclate Dimethandrolone dodecylcarbonate Dimethandrolone undecanoate Dimethisterone Dimethyltrienolone Ethisterone Ethyldienolone Ethylestrenol (ethylnandrol) Ethynerone Etonogestrel Etynodiol Etynodiol diacetate Gestodene Gestrinone Levonorgestrel Levonorgestrel butanoate Lynestrenol Methyldienolone Metribolone (R-1881) Metynodiol Metynodiol diacetate Methoxydienone (methoxygonadiene) Mibolerone Nandrolone Nandrolone esters (e.g., nandrolone decanoate, nandrolone phenylpropionate) Norelgestromin Norethisterone (norethindrone) Norethisterone acetate Norethisterone acetate oxime Norethisterone enanthate Noretynodrel Norgesterone Norgestimate Norgestrel Norgestrienone Normethandrone (methylestrenolone, normethandrolone, normethisterone) Norvinisterone Oxendolone Quingestanol Quingestanol acetate Tetrahydrogestrinone Tibolone Tigestol Tosagestin Trenbolone (trienolone) Trestolone Trestolone acetate Spirolactone derivatives: Canrenoic acid Canrenone Drospirenone Mespirenone Potassium canrenoate SC-5233 SC-8109 Spironolactone Spirorenone Non-steroidal: 3,8-Dihydrodiligustilide Riligustilide Tanaproget ZM-182345

Mixed (SPRMs)	Apigenin Asoprisnil Asoprisnil ecamate Guggulsterone Kaempferol J1042 LG-120838 Naringenin PRA-910 Syringic acid Telapristone Antagonistic: Mifepristone Org-31710 Org-33628 Ulipristal acetate ZK-137316

Antagonists	3α-Hydroxytibolone 3β-Hydroxytibolone Aglepristone Lilopristone Lonaprisan Onapristone Toripristone Valproic acid Vilaprisan Zanoterone ZM-150271 ZM-172406

mPRs
(PAQRs)

Agonists	5α-Dihydroprogesterone 5β-Dihydroprogesterone 11-Deoxycorticosterone 17α-Hydroxyprogesterone 17α,21-Dihydroxyprogesterone 21-Hydroxyprogesterone Allopregnanolone Mifepristone Pregnenolone Progesterone

Antagonists	Mifepristone

See also: Androgenics • Estrogenics • Glucocorticoidics • Mineralocorticoidics • Steroid hormone metabolism modulators

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