Fosdagrocorat

Fosdagrocorat
Clinical data
Other namesPF-04171327; PF-4171327; Dagrocorat 2-(dihydrogen phosphate); Dagrocorat dihydrogen phosphate
Drug classSelective glucocorticoid receptor modulator
Identifiers
  • [(2R,4aS,10aR)-4a-Benzyl-7-[(2-methylpyridin-3-yl)carbamoyl]-2-(trifluoromethyl)-1,3,4,9,10,10a-hexahydrophenanthren-2-yl] dihydrogen phosphate
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC29H30F3N2O5P
Molar mass574.537 g·mol−1
3D model (JSmol)
  • CC1=C(C=CC=N1)NC(=O)C2=CC3=C(C=C2)[C@@]4(CC[C@@](C[C@H]4CC3)(C(F)(F)F)OP(=O)(O)O)CC5=CC=CC=C5
  • InChI=1S/C29H30F3N2O5P/c1-19-25(8-5-15-33-19)34-26(35)22-10-12-24-21(16-22)9-11-23-18-28(29(30,31)32,39-40(36,37)38)14-13-27(23,24)17-20-6-3-2-4-7-20/h2-8,10,12,15-16,23H,9,11,13-14,17-18H2,1H3,(H,34,35)(H2,36,37,38)/t23-,27+,28-/m1/s1
  • Key:BVXLAHSJXXSWFF-KEKPKEOLSA-N

Fosdagrocorat (developmental code names PF-04171327 and PF-4171327; also known as dagrocorat 2-(dihydrogen phosphate)) is a nonsteroidal but steroid-like selective glucocorticoid receptor modulator (SGRM) which was under development for the treatment of rheumatoid arthritis but was never marketed.[1][2][3][4] It is the C2 dihydrogen phosphate ester of dagrocorat, and acts as a prodrug of dagrocorat with improved pharmacokinetics.[5][6] The drug reached phase II clinical trials prior to the discontinuation of its development.[1][3][4]

See also

References

  1. ^ a b "Fosdagrocorat - AdisInsight". adisinsight.springer.com.
  2. ^ International Nonproprietary Names for Pharmaceutical Substances (INN)
  3. ^ a b Yoshioka H, Yamada A, Nishiyama Y, Kagechika H, Hashimoto Y, Fujii S (2017). "Development of nonsteroidal glucocorticoid receptor modulators based on N-benzyl-N-(4-phenoxyphenyl)benzenesulfonamide scaffold". Bioorg. Med. Chem. 25 (13): 3461–3470. doi:10.1016/j.bmc.2017.04.032. PMID 28506584.
  4. ^ a b Strehl C, van der Goes MC, Bijlsma JW, Jacobs JW, Buttgereit F (2017). "Glucocorticoid-targeted therapies for the treatment of rheumatoid arthritis". Expert Opin Investig Drugs. 26 (2): 187–195. doi:10.1080/13543784.2017.1276562. PMID 28043173. S2CID 2306241.
  5. ^ Miyoshi S, Hey-Hadavi J, Nagaoka M, Tammara B (2016). "Pharmacokinetics and food-effect of fosdagrocorat (PF-04171327), a dissociated agonist of the glucocorticoid receptor, in healthy adult Caucasian and Japanese subjects". Int J Clin Pharmacol Ther. 54 (12): 966–976. doi:10.5414/CP202659. PMID 27781421.
  6. ^ Stock T, Fleishaker D, Wang X, Mukherjee A, Mebus C (2017). "Improved disease activity with fosdagrocorat (PF-04171327), a partial agonist of the glucocorticoid receptor, in patients with rheumatoid arthritis: a Phase 2 randomized study". Int J Rheum Dis. 20 (8): 960–970. doi:10.1111/1756-185X.13053. PMC 6084298. PMID 28328159.



Stub icon

This hormonal preparation article is a stub. You can help Wikipedia by expanding it.

Read other articles:

Idol (2019)

Idol우상 Ficha técnicaDirección Lee Su-jinGuion Lee Su-jinMúsica Kim Tae-seongSonido Lee Sung-juneKo Dong-hunMaquillaje Lee Jeong-sookFotografía Son Won-hoVestuario Kim Ha-kyungProtagonistas Han Suk-kyuSeol Gyeong-guCheon U-huiYoo Seung-mokHyun Bong-sikKang Mal-geumKim Seong-nyeoSeo Joo-heeKim Myung-gonJo Byung-gyu Ver todos los créditos (IMDb)Datos y cifrasPaís Corea del SurAño 2019Estreno 20 de marzo de 2019Género suspensoDuración 144 minutosIdioma(s) coreanoCompañíasRecaudaci...

 

Templo de Na Tcha

Templo de Na Tcha 大三巴哪吒廟 Templo de Na Tcha Tipo Templo taoísta Fim da construção 1888[1] Restauro 1995-2000[1] Proprietário atual Instituto CulturalGoverno da Região Administrativa Especial de Macau Património Mundial Critérios ii, iii, iv, vi Ano 15 de julho de 2005 Referência 1110 en fr es Geografia País  China Região administrativa especial Macau Freguesia Santo António Coordenadas 22° 11' 52 N 113° 32' 26 E Templo de Na TchaGeolocalização no...

 

Buku harian

Artikel ini bukan mengenai Buku Harian. Buku harian Mahó oleh Kapten Joan Roca Vinent Buku harian (bahasa Inggris: diary) berasal dari bahasa Latin yaitu diarium (diaria) yang akar katanya diumus, artinya masukan sehari-hari (memasukkan atau menulis setiap hari) tentang sesuatu yang terjadi atau peristiwa dalam sehari yaitu 24 jam. Yang dimaksud peristiwa di sini bersifat sangat pribadi. Dalam bahasa Perancis Kuno, diary disebut sebagai jour yang kemudian menjadi journal atau jurnal yang mem...

الجدول الزمني للنساء في الحرب والخدمة العسكرية في الولايات المتحدة، 2000-2010

هذه المقالة يتيمة إذ تصل إليها مقالات أخرى قليلة جدًا. فضلًا، ساعد بإضافة وصلة إليها في مقالات متعلقة بها. (يونيو 2019) يسرد هذا المقال الأحداث التي شاركت فيها النساء في الحروب والعسكرية في الولايات المتحدة من عام 2000 حتى عام 2010. الأحداث 2000 الربيع: كاثلين ماكغراثأول امرأة تقود ...

 

Mephistopheles

Demon in German folklore For other uses, see Mephistopheles (disambiguation). Mephistopheles flying over Wittenberg, in a lithograph by Eugène Delacroix Mephistopheles[a] (/ˌmɛfɪˈstɒfɪˌliːz/, German pronunciation: [mefɪˈstoːfɛlɛs]), also known as Mephisto,[1] is a demon featured in German folklore. He originally appeared in literature as the demon in the Faust legend and has since become a stock character appearing in other works of arts and popular cultu...

 

Pogona

Genus of lizards commonly known as bearded dragons Pogona Pogona vitticeps P. vitticeps – detail of head Scientific classification Domain: Eukaryota Kingdom: Animalia Phylum: Chordata Class: Reptilia Order: Squamata Suborder: Iguania Family: Agamidae Subfamily: Amphibolurinae Genus: PogonaStorr, 1982[1] Species Pogona barbata Pogona henrylawsoni Pogona microlepidota Pogona minor Pogona mitchelli Pogona nullarbor Pogona vitticeps Pogona is a genus of reptiles containing eight lizard ...

Télé-Liban

Télé LibanCaractéristiquesCréation 30 décembre 1977Propriétaire Télé Liban S.A.LFormat d'image 16/9, 4/3Langue Arabe, français et anglaisPays LibanStatut Généraliste nationale publiqueSiège social Tour Télé Liban, 11 Rue Al-Rachidine, Quartier Tallet-El-Khayyat, 4848 BeyrouthAncien nom Canal 7 (1959-1977) TL1 (1977-1991) Télé Liban (1991-présent)Chaîne sœur Le NeufSite web site officielDiffusionAire Monde entierDiffusion satellite, câble, analogique et Web.modifier - modif...

 

No Reservations (film)

2007 American filmNo ReservationsTheatrical release posterDirected byScott HicksWritten byCarol FuchsBased onMostly Marthaby Sandra NettelbeckProduced byKerry HeysenSergio AgueroStarring Catherine Zeta-Jones Aaron Eckhart Abigail Breslin Patricia Clarkson CinematographyStuart DryburghEdited byPip KarmelMusic byPhilip GlassProductioncompaniesCastle Rock EntertainmentVillage Roadshow PicturesDistributed byWarner Bros. PicturesRelease dateJuly 27, 2007 (2007-07-27)Running time104 ...

 

Grace Hickling

English ornithologist This article relies largely or entirely on a single source. Relevant discussion may be found on the talk page. Please help improve this article by introducing citations to additional sources.Find sources: Grace Hickling – news · newspapers · books · scholar · JSTOR (June 2020) Grace Hickling MBE (10 August 1908 – 30 December 1986) was an English ornithologist known for studying wildlife on the Farne Islands, in the North Sea...

Betting on Zero

2016 film by Ted Braun Betting on ZeroDirected byTed BraunProduced by Glen Zipper Devin Adair CinematographyBuddy SquiresEdited byLeonard FeinsteinMusic byPete AnthonyProductioncompaniesZipper Brothers Films, Biltmore FilmsDistributed byGunpowder & SkyRelease date April 14, 2016 (2016-04-14) (Tribeca Film Festival) Running time98 minutesCountryUnited StatesLanguageEnglish Betting on Zero is a 2016 American documentary directed by Ted Braun. It investigates the allegatio...

 

Russian Cultural Centre (Lviv)

Russian Cultural Center in Lviv (Ukrainian: Російський культурний центр у Львові, Russian: Русский культурный центр во Львове) was an organization of Russian culture in Lviv, the only organization in this interest in West-Ukraine. The center was the first of its kind[1] to be opened in the USSR and it was the only one for a long time in the territory of Ukraine. In October 2016 the center was evicted by the Lviv regional co...

 

C.D. Jorge Wilstermann

Jorge WilstermannNama lengkapClub Deportivo Jorge WilstermannJulukanEl Equipo Aviador, Wilster, Hercules, Rojo del valleBerdiriNovember 24, 1949StadionEstadio Félix Capriles,Cochabamba, Bolivia(Kapasitas: 32,000 [1])Ketua Angel CamperoManajer Néstor ClausenLigaLiga de Fútbol Profesional BolivianoLiga Nacional B - 2011–123rd Promosi Kostum kandang Kostum tandang Kostum ketiga Club Deportivo Jorge Wilstermann adalah tim sepak bola profesional asal Bolivia yang kini berkompetisi di Liga de ...

Mamie Gummer

American actress (born 1983) Mamie GummerGummer in 2015BornMary Willa Gummer (1983-08-03) August 3, 1983 (age 40)New York City, U.S.Alma materNorthwestern UniversityOccupationActressYears active1986–presentSpouses Benjamin Walker ​ ​(m. 2011; div. 2013)​ Mehar Sethi ​(m. 2019)​ Children2Parent(s)Don GummerMeryl StreepRelatives Henry Wolfe Gummer (brother) Grace Gummer (sister) Louisa Jacobson (sister...

 

J. Joseph Garrahy

American governor of Rhode Island J. Joseph Garrahy69th Governor of Rhode IslandIn officeJanuary 4, 1977 – January 1, 1985LieutenantThomas R. DiLuglioPreceded byPhilip NoelSucceeded byEdward D. DiPrete61st Lieutenant Governor of Rhode IslandIn officeJanuary 7, 1969 – January 4, 1977GovernorFrank LichtPhilip NoelPreceded byJoseph O'Donnell Jr.Succeeded byThomas R. DiLuglioMember of theRhode Island SenateIn office1963–1969 Personal detailsBornJohn Joseph Garrahy(...

 

Free music

Music in the public domain or under a free license For other uses, see Free improvisation. The crossed out copyright symbol with a musical note on the right hand side is the free music symbol, signifying a lack of copyright restrictions on music. It may be used in the abstract, or applied to a sound recording or musical composition. Free music or libre music is music that, like free software, can freely be copied, distributed and modified for any purpose. Thus free music is either in the publ...

Ernest Doudart de Lagrée

Ernest Doudart de Lagrée, from Voyage d'exploration en Indo-Chine Ernest Marc Louis de Gonzague Doudart de Lagrée (French pronunciation: [ɛʁnɛst dudaʁ də laɡʁe]; March 31, 1823 – March 12, 1868) was the leader of the French Mekong Expedition of 1866-1868.[1] He was born in Saint-Vincent-de-Mercuze near Grenoble, France, and graduated from the École Polytechnique.[2] He joined the navy and served in the Crimean War, then took up a post in Indochina in th...

 

Iman (model)

Somali model and actress ImanIimaanIman in 1996BornZara Mohamed Abdulmajid (1955-07-25) 25 July 1955 (age 68)Mogadishu, Banaadir, Trust Territory of SomalilandOccupationsModelactressbusinesswomanYears active1975–presentSpouses Hassan ​ ​(m. 1973; div. 1975)​ Spencer Haywood ​ ​(m. 1977; div. 1987)​ David Bowie ​ ​(m. 1992; died 2016)​Child...

 

جورج حاوي

جورج حاوي معلومات شخصية الميلاد 5 نوفمبر 1938  بتغرين  الوفاة 21 يونيو 2005 (66 سنة)   بيروت  سبب الوفاة محاولة قتل  [لغات أخرى]‏  مواطنة لبنان  الحياة العملية المهنة سياسي  الحزب الحزب الشيوعي اللبناني (1955–2000)  تعديل مصدري - تعديل   جورج حاوي (5 تشرين ال...

Славянская мифология

Эта статья — о мифологических представлениях. О дохристианских верованиях, культах и ритуалах см. Славянское язычество. Запрос «Русская мифология» перенаправляется сюда. На эту тему нужно создать отдельную статью. Запрос «Украинская мифология» перенаправля...

 

MARUV

У Вікіпедії є статті про інших людей із прізвищем Корсун. Не плутати з MARU. MARUV Основна інформаціяПовне ім'я Анна Борисівна КорсунДата народження 15 лютого 1991(1991-02-15) (33 роки)Місце народження Павлоград, Дніпропетровська область  УкраїнаРоки активності 2013 — дотеперГром...

 

Strategi Solo vs Squad di Free Fire: Cara Menang Mudah!