General Information of Drug (ID: DMKA705)

Drug Name
PGL-2001 Drug Info
Synonyms Steroid sulfatase inhibitor (endometriosis), PregLem
Indication
Disease Entry ICD 11 Status REF
Endometriosis GA10 Phase 2 [1]
Cross-matching ID
PubChem CID
6918339
CAS Number
CAS 172377-52-5
TTD Drug ID
DMKA705

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Investigative Drug(s)
Drug(s) Targeting Steryl-sulfatase (STS)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Tranilast DME5Y64 Allergic rhinitis CA08.0 Approved [3]
Coumate DMVKW0N Breast cancer 2C60-2C65 Phase 2 [4]
STX-140 DMJK5CT Osteoporosis FB83.0 Phase 2 [5]
PGL-2 DMJTYO4 Endometriosis GA10 Phase 2 [2]
STX 64 DMJAPRK Prostate cancer 2C82.0 Phase 1 [6]
B-Octylglucoside DMMO75G Discovery agent N.A. Investigative [7]
EMATE DMFQX1U Discovery agent N.A. Investigative [8]
Sulfamic acid 2-nonyl-4-oxo-4H-chromen-6-yl ester DMM70K1 Discovery agent N.A. Investigative [9]
Estradiol 17-O-sulfamate DM7K14V Discovery agent N.A. Investigative [5]
4-Sulfamoyloxy-benzoic acid pentyl ester DMZIFW7 Discovery agent N.A. Investigative [10]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Steryl-sulfatase (STS) TTHM0R1 STS_HUMAN Inhibitor [2]

References

1 ClinicalTrials.gov (NCT01631981) PGL2001 Proof of Concept Study in Symptomatic Endometriosis. U.S. National Institutes of Health.
2 Synergistic effects of E2MATE and norethindrone acetate on steroid sulfatase inhibition: a randomized phase I proof-of-principle clinical study in women of reproductive age. Reprod Sci. 2014 Oct;21(10):1256-65.
3 Review of estrone sulfatase and its inhibitors--an important new target against hormone dependent breast cancer. Curr Med Chem. 2002 Jan;9(2):263-73.
4 Highly potent first examples of dual aromatase-steroid sulfatase inhibitors based on a biphenyl template. J Med Chem. 2010 Mar 11;53(5):2155-70.
5 2-substituted estradiol bis-sulfamates, multitargeted antitumor agents: synthesis, in vitro SAR, protein crystallography, and in vivo activity. J Med Chem. 2006 Dec 28;49(26):7683-96.
6 Phase I study of STX 64 (667 Coumate) in breast cancer patients: the first study of a steroid sulfatase inhibitor. Clin Cancer Res. 2006 Mar 1;12(5):1585-92.
7 How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
8 Thiosemicarbazones of formyl benzoic acids as novel potent inhibitors of estrone sulfatase. J Med Chem. 2007 Jul 26;50(15):3661-6.
9 Estrogenic potential of 2-alkyl-4-(thio)chromenone 6-O-sulfamates: potent inhibitors of human steroid sulfatase. J Med Chem. 2003 Nov 6;46(23):5091-4.
10 Inhibition of estrone sulfatase (ES) by alkyl and cycloalkyl ester derivatives of 4-[(aminosulfonyl)oxy] benzoic acid. Bioorg Med Chem Lett. 2004 Feb 9;14(3):605-9.