Drug Information

Drug (ID: DG00867) and It's Reported Resistant Information

• Name: Medroxyprogesterone
• Synonyms: Medroxyprogesterone; 520-85-4; Medroxyprogesteron; Medroxiprogesteronum; Medroxiprogesterona; Medroxyprogesteronum; 17-Hydroxy-6alpha-methylprogesterone; Hydroxymethylprogesterone; Medrossiprogesterone; 17alpha-Hydroxy-6alpha-methylprogesterone; 6alpha-Methyl-17alpha-hydroxyprogesterone; 6alpha-Methyl-4-pregnen-17alpha-ol-3,20-dione; 17-Hydroxy-6alpha-methyl-pregn-4-ene-3,20-dione; UNII-HSU1C9YRES; Medroxy Progesterone; U 8840; (6alpha)-17-hydroxy-6-methylpregn-4-ene-3,20-dione; HSU1C9YRES; (6S,8R,9S,10R,13S,14S,17R)-17-acetyl-17-hydroxy-6,10,13-trimethyl-2,6,7,8,9,11,12,14,15,16-decahydro-1H-cyclopenta[a]phenanthren-3-one; Pregn-4-ene-3,20-dione, 17-hydroxy-6-alpha-methyl-; MLS000069571; CHEBI:6715; 17alpha-Hydroxy-6alpha-methyl-4-pregnene-3,20-dione; SMR000058769; Medrossiprogesterone [DCIT]; NSC 27408; DSSTox_CID_16508; DSSTox_RID_79284; DSSTox_GSID_36508; Medroxyprogesteronum [INN-Latin]; Medroxiprogesterona [INN-Spanish]; Medroxyprogesterone [INN:BAN]; 17-Hydroxy-6.alpha.-methylprogesterone; 6-Dihydromegestrol; CAS-520-85-4; 17.alpha.-Hydroxy-6.alpha.-methylprogesterone; 6.alpha.-Methyl-17.alpha.-hydroxyprogesterone; HSDB 3114; 6-alpha-Methyl-17-alpha-hydroxyprogesterone; MLS002639162; EINECS 208-298-6; Farlutal inyectable (TN); Medroxyprogesterone (INN); BRN 2510965; NCGC00183122-01; CPD000058769; Pregn-4-ene-3,20-dione, 17-hydroxy-6-methyl-, (6alpha)-; Opera_ID_433; CHEMBL1390; 6alpha-Methyl-5-pregnen-17alpha-ol-3,20-dione; SCHEMBL37494; 4-08-00-02211 (Beilstein Handbook Reference); MLS001076098; MLS001424229; GTPL2879; DTXSID0036508; 17-Hydroxy-6a-methylprogesterone; HMS2052A13; HMS2230B08; HY-B0648; NSC27408; ZINC5763835; Tox21_113401; 3808AH; LMST02030176; MFCD00069474; s3635; AKOS015961681; Tox21_113401_1; CCG-101111; NC00361; MRF-0000022; NCGC00023064-04; NCGC00023064-05; AC-14528; M3113; 17; A-Hydroxy-6; A-methylprogesterone;U8840; Medroxyprogesterone acetate Related Compound B; C07119; C75441; D08166; Pregn-4-ene-3, 17-hydroxy-6.alpha.-methyl-; 520M854; A899740; Q416667; (6 )-17-Hydroxy-6-methylpregn-4-ene-3,20-dione; Medroxyprogesterone, VETRANAL(TM), analytical standard; Pregn-4-ene-3, 17-hydroxy-6-methyl-, (6.alpha.)-; Pregn-4-ene-3,20-dione, 17-hydroxy-6-methyl-, (6alpha)- (9CI); Pregn-4-ene-3,20-dione, 17-hydroxy-6-methyl-, (6-alpha)- (9CI); (6S,8R,10R,13S,17R)-17-Acetyl-17-hydroxy-6,10,13-trimethyl-1,2,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-cyclopenta[a]phenanthren-3-one; (6S,8R,9S,10R,13S,14S,17R)-17-acetyl-17-hydroxy-6,10,13-trimethyl-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-3(2H)-one; Medroxyprogesterone acetate Related Compound B, United States Pharmacopeia (USP) Reference Standard
• Indication:
  In total 1 Indication(s)
  Solid tumour/cancer [ICD-11: 2A00-2F9Z]; Approved; [1]
• Drug Resistance Disease(s):
  Disease(s) with Resistance Information Discovered by Cell Line Test for This Drug (1 diseases)
  Endometrial cancer [ICD-11: 2C76]; [1]
• Target: Progesterone receptor (PGR); PRGR_HUMAN; [1]
• Formula: C22H32O3
• IsoSMILES: C[C@H]1C[C@@H]2[C@H](CC[C@]3([C@H]2CC[C@@]3(C(=O)C)O)C)[C@@]4(C1=CC(=O)CC4)C
• InChI: 1S/C22H32O3/c1-13-11-16-17(20(3)8-5-15(24)12-19(13)20)6-9-21(4)18(16)7-10-22(21,25)14(2)23/h12-13,16-18,25H,5-11H2,1-4H3/t13-,16+,17-,18-,20+,21-,22-/m0/s1
• InChIKey: FRQMUZJSZHZSGN-HBNHAYAOSA-N
• PubChem CID: 10631
• ChEBI ID: CHEBI:6715
• TTD Drug ID: D0I2SD

Type(s) of Resistant Mechanism of This Drug

  ADTT: Aberration of the Drug's Therapeutic Target

Drug Resistance Data Categorized by Their Corresponding Diseases

ICD-02: Benign/in-situ/malignant neoplasm

Endometrial cancer [ICD-11: 2C76]

Drug Resistance Data Categorized by Their Corresponding Mechanisms

Aberration of the Drug's Therapeutic Target (ADTT)

Key Molecule: Progesterone receptor (PGR) [1]

• Molecule Alteration: Expression; Up-regulation
• Resistant Disease: Endometrial cancer [ICD-11: 2C76.1]
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: SR786 cells; Pleural effusion; Homo sapiens (Human); CVCL_1711
• In Vitro Model: IshikawaPR cells; Endometrium; Homo sapiens (Human); CVCL_2529
• Experiment for Molecule Alteration: RTPCR
• Mechanism Description: The presence of the progesterone receptor (PR) is the precondition for progesterone response and PR is a predictive marker for response of progesterone. Progesterone binds to its receptor PR-A and PR-B, subsequently inhibiting tumor growth and promoting tumor apoptosis by regulating downstream genes. Constant stimulation of progesterone reduced the expression of PGR and promoted the development of drug resistance. Thus, downregulation of PR especially PRB must be involved in progesterone resistance. However, the molecular mechanism of PGR dysfunction remains unclear.

References

• Ref 1: Comprehensive bioinformatics analysis of acquired progesterone resistance in endometrial cancer cell line .J Transl Med. 2019 Feb 27;17(1):58. doi: 10.1186/s12967-019-1814-6. 10.1186/s12967-019-1814-6