Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DMB8T5U)

• Drug Name: ONT-093 Drug Info
• Synonyms: MDR inhibitors, Ontogen; OC-144-093

Indication

Disease Entry	ICD 11	Status	REF
Solid tumour/cancer	2A00-2F9Z	Discontinued in Phase 1	[1]

• Cross-matching ID:
  PubChem CID: 6450807
  CAS Number: CAS 216227-54-2
  TTD Drug ID: DMB8T5U

Molecule-Related Drug Atlas

Drug(s) Targeting Multidrug resistance protein 1 (ABCB1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
EDP-322	DMWTVM1	Bacterial infection	1A00-1C4Z	Phase 1	[3]
W-198	DMJ2R69	Solid tumour/cancer	2A00-2F9Z	Phase 1	[4]
LY335979	DM2KITF	Acute myeloid leukaemia	2A60	Discontinued in Phase 3	[5]
CBT-1	DM097UP	Non-small-cell lung cancer	2C25.Y	Discontinued in Phase 3	[6]
Biricodar	DM65JCM	Ovarian cancer	2C73	Discontinued in Phase 2	[7]
Tariquidar	DMJG7VP	Adrenocortical carcinoma	2D11.Z	Discontinued in Phase 2	[8]
Elacridar	DMURVE8	Solid tumour/cancer	2A00-2F9Z	Discontinued in Phase 1	[9]
TRISMETHOXYRESVERATROL	DM6USPC	Discovery agent	N.A.	Investigative	[10]
[1,1':2',1'']-terphenyl-4,3'',5''-triol	DMVOY4D	Discovery agent	N.A.	Investigative	[10]
XR-9456	DMTUFI1	Discovery agent	N.A.	Investigative	[11]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Multidrug resistance protein 1 (ABCB1)	TT3OT40	MDR1_HUMAN	Inhibitor	[2]

References

• [1] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800011621)
• [2] A phase I pharmacokinetic study of the P-glycoprotein inhibitor, ONT-093, in combination with paclitaxel in patients with advanced cancer. Invest New Drugs. 2005 Aug;23(4):311-5.
• [3] In vitro activities of the novel bicyclolides modithromycin (EDP-420, EP-013420, S-013420) and EDP-322 against MDR clinical Neisseria gonorrhoeae isolates and international reference strains. J Antimicrob Chemother. 2015 Jan;70(1):173-7.
• [4] Mechanisms of tetrandrine and 5-bromotetrandrine in reversing multidrug resistance may relate to down-regulation of multidrug resistance associated protein 7 expression. Zhongguo Shi Yan Xue Ye Xue Za Zhi. 2012 Jun;20(3):558-63.
• [5] A Phase I trial of a potent P-glycoprotein inhibitor, zosuquidar trihydrochloride (LY335979), administered intravenously in combination with doxoru... Clin Cancer Res. 2004 May 15;10(10):3265-72.
• [6] A pharmacodynamic study of the P-glycoprotein antagonist CBT-1 in combination with paclitaxel in solid tumors. Oncologist.2012;17(4):512.
• [7] ClinicalTrials.gov (NCT00003847) VX-710, Doxorubicin, and Vincristine for the Treatment of Patients With Recurrent Small Cell Lung Cancer. U.S. National Institutes of Health.
• [8] Inhibition of P-glycoprotein (ABCB1)- and multidrug resistance-associated protein 1 (ABCC1)-mediated transport by the orally administered inhibitor, CBT-1((R)).Biochem Pharmacol.2008 Mar 15;75(6):1302-12.
• [9] 2-[(3-Methoxyphenylethyl)phenoxy]-based ABCB1 inhibitors: effect of different basic side-chains on their biological properties. J Med Chem. 2008 Dec 11;51(23):7602-13.
• [10] Identification of a terphenyl derivative that blocks the cell cycle in the G0-G1 phase and induces differentiation in leukemia cells. J Med Chem. 2006 May 18;49(10):3012-8.
• [11] Functional assay and structure-activity relationships of new third-generation P-glycoprotein inhibitors. Bioorg Med Chem. 2008 Mar 1;16(5):2448-62.