General Information of DTT (ID: TTUV8G9)

DTT Name Progesterone receptor (PGR) DTT Info
Gene Name PGR

Molecule-Related Drug & Molecule List

Molecule-Related Drug List
Molecule Type:
DTT
DTP
DME
Drug Status:
Discontinued Drug(s)
Approved Drug(s)
Clinical Trial Drug(s)
Investigative Drug(s)
12 Approved Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Desogestrel DM27U4Y Contraception QA21 Approved [1]
Dydrogesterone DMAKIDV Menstrual disorder GA20.3 Approved [2]
Ethynodiol Diacetate DMZM84R Contraception QA21 Approved [3]
Etonogestrel DMKA8J4 Contraception QA21 Approved [4]
Levonorgestrel DM1DP7T Atypical endometrial hyperplasia Approved [5]
Medroxyprogesterone DMBGWPH Solid tumour/cancer 2A00-2F9Z Approved [2]
Megestrol DMDH9KX Breast cancer 2C60-2C65 Approved [6]
Norethindrone DMTY169 Acne vulgaris ED80 Approved [7]
Norgestimate DMYP4XC Acne vulgaris ED80 Approved [4]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [8]
Segesterone acetate; ethinyl estradiol DMFEGB0 Contraception QA21 Approved [9]
Ulipristal DMBNI20 Contraception QA21 Approved [10]
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⏷ Show the Full List of 12 Approved Drug(s)
11 Clinical Trial Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Nestorone DMVP7HI Endometriosis GA10 Phase 3 [11]
NPC-01 DMMC3Y8 Dysmenorrhea GA34.3 Phase 3 [12]
BAY 86-5044 DMRZLU4 Breast cancer 2C60-2C65 Phase 2 [13]
MK-8342 DMD6E5W Contraception QA21 Phase 2 [14]
ONAPRISTONE DMT6E5N Breast cancer 2C60-2C65 Phase 2 [15]
S-PRAnt DMFAO5G Uterine fibroids 2E86.0 Phase 2 [16]
Telapristone DM9AWSO Endometriosis GA10 Phase 2 [17]
Tosagestin DM2HDTM Contraception QA21 Phase 2 [18]
Vilaprisan DME7VZD Endometriosis GA10 Phase 2 [19]
Virexxa DMEXMV5 Endometrial cancer 2C76 Phase 2 [14]
PF-2413873 DMCOUHT Endometriosis GA10 Phase 1 [20]
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⏷ Show the Full List of 11 Clinical Trial Drug(s)
4 Discontinued Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Asoprisnil DM4BV2W Endometriosis GA10 Discontinued in Phase 3 [21]
Org-31710 DMZKTU5 Contraception QA21 Discontinued in Phase 1 [22]
BAY-39-9624 DMPUG18 Osteoporosis FB83.0 Terminated [23]
RU-46556 DM8B1DH Endometrial cancer 2C76 Terminated [24]
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25 Investigative Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
1-Benzyl-3-phenylquinazoline-2,4(1H,3H)-dione DMV7UC0 Discovery agent N.A. Investigative [25]
2,2,4-Trimethyl-6-phenyl-1,2-dihydro-quinoline DMP9ECK Discovery agent N.A. Investigative [26]
2-(4-Amino-3'-chloro-biphenyl-3-yl)-propan-2-ol DMSHPCW Discovery agent N.A. Investigative [27]
3,3-dimethyl-5-m-tolyl-2,3-dihydro-1H-inden-1-one DMUS0A4 Discovery agent N.A. Investigative [28]
3-(3,3-dimethyl-2-oxoindolin-5-yl)benzonitrile DMSHORK Discovery agent N.A. Investigative [29]
3-Phenyl-1-propylquinazoline-2,4(1H,3H)-dione DMEG3YX Discovery agent N.A. Investigative [25]
4-(2,4-diethyl-1H-pyrrol-3-yloxy)benzonitrile DMBLAI1 Discovery agent N.A. Investigative [30]
5,N-Dihydroxythalidomide DM3MSZN Discovery agent N.A. Investigative [25]
5-(2-oxoindolin-5-yl)-1H-pyrrole-2-carbonitrile DMR7OHB Discovery agent N.A. Investigative [29]
6-(3-Nitro-phenyl)-3H-benzothiazol-2-one DM83VN6 Discovery agent N.A. Investigative [31]
AL-43 DMLEDHR Discovery agent N.A. Investigative [32]
GSK-008A DMC2ZF6 Gynecological disease GA6Z Investigative [14]
GSK-1564023A DMKN76P Discovery agent N.A. Investigative [33]
GSK-325971A DM1865H Discovery agent N.A. Investigative [33]
GTPL8662 DMZQETV Discovery agent N.A. Investigative [34]
Lecanindole D DMZ7OHP Discovery agent N.A. Investigative [35]
LGD-5552 DM67KWM Discovery agent N.A. Investigative [36]
ORG2058 DMH1M6N Discovery agent N.A. Investigative [14]
PF-02367982 DMZ5JNT Endometriosis GA10 Investigative [30]
Tanaproget DMQCW7V Estrogen deficiency FB83.0Y Investigative [37]
WAY-255348 DMSLNWA Solid tumour/cancer 2A00-2F9Z Investigative [29]
ZK-112993 DM8JN45 Discovery agent N.A. Investigative [38]
ZK-114043 DMBCPKE Discovery agent N.A. Investigative [39]
ZK-136798 DMCQYBE Discovery agent N.A. Investigative [40]
[3H]methyltrienolone DMTSGOW Discovery agent N.A. Investigative [41]
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⏷ Show the Full List of 25 Investigative Drug(s)
Molecule Interaction Atlas

References

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2 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.
3 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.
4 Pharmacological profile of progestins. Maturitas. 2008 Sep-Oct;61(1-2):151-7.
5 Met909 plays a key role in the activation of the progesterone receptor and also in the high potency of 13-ethyl progestins. Mol Pharmacol. 2009 Jun;75(6):1317-24.
6 Focus on anastrozole and breast cancer. Curr Med Res Opin. 2003;19(8):683-8.
7 Progesterone receptor ligand binding pocket flexibility: crystal structures of the norethindrone and mometasone furoate complexes. J Med Chem. 2004 Jun 17;47(13):3381-7.
8 Clinical pipeline report, company report or official report of lipocine.
9 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89.
10 Mullard A: 2010 FDA drug approvals. Nat Rev Drug Discov. 2011 Feb;10(2):82-5.
11 Efficacy of the selective progesterone receptor agonist Nestorone for chronic experimental autoimmune encephalomyelitis. J Neuroimmunol. 2014 Nov 15;276(1-2):89-97.
12 ClinicalTrials.gov (NCT01246791) Pharmacokinetics of NPC-01 After Single Oral Administration in Healthy Female Volunteers. U.S. National Institutes of Health.
13 Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist. J Med Chem. 2000 Dec 28;43(26):5010-6.
14 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 627).
15 Onapristone, a progesterone receptor antagonist, as first-line therapy in primary breast cancer. Eur J Cancer. 1999 Feb;35(2):214-8.
16 BAY 1002670: a novel, highly potent and selective progesterone receptor modulator for gynaecological therapies. Hum Reprod. 2013 Aug;28(8):2253-64.
17 In vitro antiprogestational/antiglucocorticoid activity and progestin and glucocorticoid receptor binding of the putative metabolites and synthetic derivatives of CDB-2914, CDB-4124, and mifepristone. J Steroid Biochem Mol Biol. 2004 Mar;88(3):277-88.
18 Effects of progestins on the proliferation of estrogen-dependent human breast cancer cells under growth factor-defined conditions. J Steroid Biochem Mol Biol. 1992 Jun;42(5):457-65.
19 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800033939)
20 Unusual base-catalyzed exchange in the synthesis of deuterated PF-2413873. Journal of Labelled Compounds. 08/2009; 52(10):435 - 442.
21 New drugs in development for the treatment of endometriosis. Expert Opin Investig Drugs. 2008 Aug;17(8):1187-202.
22 Progesterone receptor antagonists Org 31710 and RU 486 increase apoptosis in human periovulatory granulosa cells. Fertil Steril. 2001 Dec;76(6):1225-31.
23 Bayer is seeking an exclusive licensee for its end-of-Phase I progestinagonist Bay 39-9624. Thepharmaletter. 29-04-2002.
24 New analogues of mifepristone with more dissociated antiprogesterone activities. J Steroid Biochem. 1989;34(1-6):413-7.
25 Progesterone receptor antagonists with a 3-phenylquinazoline-2,4-dione/2-phenylisoquinoline-1,3-dione skeleton. Bioorg Med Chem. 2008 Jul 15;16(14):7046-54.
26 Discovery and preliminary SAR studies of a novel, nonsteroidal progesterone receptor antagonist pharmacophore. J Med Chem. 1998 Aug 27;41(18):3461-6.
27 Potent nonsteroidal progesterone receptor agonists: synthesis and SAR study of 6-aryl benzoxazines. Bioorg Med Chem Lett. 2002 Mar 11;12(5):787-90.
28 5-Aryl indanones and derivatives as non-steroidal progesterone receptor modulators. Bioorg Med Chem Lett. 2009 Dec 1;19(23):6666-9.
29 Design, synthesis, and SAR of new pyrrole-oxindole progesterone receptor modulators leading to 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-... J Med Chem. 2008 Mar 27;51(6):1861-73.
30 Optimisation of a pyrazole series of progesterone antagonists; Part 1. Bioorg Med Chem Lett. 2010 Jun 1;20(11):3384-6.
31 Synthesis and structure-activity relationship of novel 6-aryl-1,4-dihydrobenzo[d][1,3]oxazine-2-thiones as progesterone receptor modulators leading... J Med Chem. 2005 Aug 11;48(16):5092-5.
32 Nonsteroidal selective glucocorticoid modulators: the effect of C-10 substitution on receptor selectivity and functional potency of 5-allyl-2,5-dih... J Med Chem. 2003 Mar 13;46(6):1016-30.
33 The identification a novel, selective, non-steroidal, functional glucocorticoid receptor antagonist. Bioorg Med Chem Lett. 2010 Apr 1;20(7):2340-3.
34 A new strategy for selective targeting of progesterone receptor with passive antagonists. Mol Endocrinol. 2013 Jun;27(6):909-24.
35 The lecanindoles, nonsteroidal progestins from the terrestrial fungus Verticillium lecanii 6144. J Nat Prod. 2009 Nov;72(11):1944-8.
36 Antiinflammatory glucocorticoid receptor ligand with reduced side effects exhibits an altered protein-protein interaction profile. Proc Natl Acad Sci U S A. 2007 Dec 4;104(49):19244-9.
37 The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
38 Tumor-inhibiting potential of ZK 112.993, a new progesterone antagonist, in hormone-sensitive, experimental rodent and human mammary tumors.Anticancer Res.1990 May-Jun;10(3):683-7.
39 Progesterone inhibits glucocorticoid-dependent aromatase induction in human adipose fibroblasts. J Endocrinol. 1998 Sep;158(3):401-7.
40 The antiovulatory activity of progesterone antagonists is not correlated to their antiprogestational potency in the rat. J Steroid Biochem Mol Biol. 1996 Sep;59(1):75-82.
41 How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.