Details of the Drug Combination

General Information of Drug Combination (ID: DCQ01SW)

• Drug Combination Name: Terameprocol + FORMESTANE
• Indication: Cutaneous melanoma; Status: Investigative [1]
• Component Drugs:
  Terameprocol (DMC3P45): Small molecular drug
  FORMESTANE (DMWIDJK): Small molecular drug
• High-throughput Screening Result:
  Testing Cell Line: SK-MEL-28
  Zero Interaction Potency (ZIP) Score: 2.21
  Bliss Independence Score: 3.73
  Loewe Additivity Score: 2.84
  LHighest Single Agent (HSA) Score: 0.89

Molecular Interaction Atlas of This Drug Combination

Indication(s) of Terameprocol

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

Terameprocol Interacts with 1 DTT Molecule(s)

DTT Name	DTT ID	UniProt ID	Mode of Action	REF
Transcription factor Sp1 (SP1)	TTZEP6S	SP1_HUMAN	Modulator	[2]

Indication(s) of FORMESTANE

Disease Entry	ICD 11	Status	REF
Breast cancer	2C60-2C65	Withdrawn from market	[3]

FORMESTANE Interacts with 1 DTT Molecule(s)

DTT Name	DTT ID	UniProt ID	Mode of Action	REF
Aromatase (CYP19A1)	TTSZLWK	CP19A_HUMAN	Inhibitor	[4]

FORMESTANE Interacts with 5 DOT Molecule(s)

DOT Name	DOT ID	UniProt ID	Mode of Action	REF
Adenylate kinase isoenzyme 1 (AK1)	OT614AR3	KAD1_HUMAN	Increases ADR	[5]
Aromatase (CYP19A1)	OTZ6XF74	CP19A_HUMAN	Decreases Activity	[6]
17-beta-hydroxysteroid dehydrogenase type 1 (HSD17B1)	OT6EBDHM	DHB1_HUMAN	Decreases Activity	[7]
Estrogen receptor (ESR1)	OTKLU61J	ESR1_HUMAN	Increases Expression	[8]
Androgen receptor (AR)	OTUBKAZZ	ANDR_HUMAN	Increases Expression	[8]

Test Results of This Drug Combination in Other Disease Systems

Indication	DrugCom ID	Cell Line	Status	REF
Adult acute myeloid leukemia	DCI7XJI	HL-60(TB)	Investigative	[9]
Astrocytoma	DCDK4FE	U251	Investigative	[9]
Childhood T acute lymphoblastic leukemia	DCQ06SU	CCRF-CEM	Investigative	[9]
Clear cell renal cell carcinoma	DCMXN65	786-0	Investigative	[9]
Clear cell renal cell carcinoma	DC4CMM2	CAKI-1	Investigative	[9]
Glioma	DCBT0OR	SF-295	Investigative	[9]
Plasma cell myeloma	DCI323K	RPMI-8226	Investigative	[9]
Colon adenocarcinoma	DCZW91A	COLO 205	Investigative	[10]
Adenocarcinoma	DCQ5KCF	OVCAR3	Investigative	[1]
Adenocarcinoma	DCTGLTL	HCT116	Investigative	[1]
Adenocarcinoma	DCQEH2M	SW-620	Investigative	[1]
Adenocarcinoma	DC23I9R	HT29	Investigative	[1]
Amelanotic melanoma	DCU7YSO	M14	Investigative	[1]
High grade ovarian serous adenocarcinoma	DCOY3T3	NCI\\/ADR-RES	Investigative	[1]
Large cell lung carcinoma	DCCH7JN	NCI-H460	Investigative	[1]
Malignant melanoma	DCUOXAK	UACC62	Investigative	[1]
Minimally invasive lung adenocarcinoma	DCP5MTL	NCI-H322M	Investigative	[1]
Prostate carcinoma	DCCJYXM	PC-3	Investigative	[1]

References

• [1] Loss of function mutations in VARS encoding cytoplasmic valyl-tRNA synthetase cause microcephaly, seizures, and progressive cerebral atrophy.Hum Genet. 2018 Apr;137(4):293-303. doi: 10.1007/s00439-018-1882-3. Epub 2018 Apr 24.
• [2] Terameprocol, a novel site-specific transcription inhibitor with anticancer activity. IDrugs. 2008 Mar;11(3):204-14.
• [3] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [4] The taiwaniaquinoids: a review. J Nat Prod. 2010 Feb 26;73(2):284-98.
• [5] ADReCS-Target: target profiles for aiding drug safety research and application. Nucleic Acids Res. 2018 Jan 4;46(D1):D911-D917. doi: 10.1093/nar/gkx899.
• [6] Screening of selected pesticides for inhibition of CYP19 aromatase activity in vitro. Toxicol In Vitro. 2000 Jun;14(3):227-34.
• [7] Mammalian lignans and genistein decrease the activities of aromatase and 17beta-hydroxysteroid dehydrogenase in MCF-7 cells. J Steroid Biochem Mol Biol. 2005 Apr;94(5):461-7.
• [8] Androgen- and estrogen-receptor mediated activities of 4-hydroxytestosterone, 4-hydroxyandrostenedione and their human metabolites in yeast based assays. Toxicol Lett. 2018 Aug;292:39-45. doi: 10.1016/j.toxlet.2018.04.026. Epub 2018 Apr 24.
• [9] Recurrent recessive mutation in deoxyguanosine kinase causes idiopathic noncirrhotic portal hypertension.Hepatology. 2016 Jun;63(6):1977-86. doi: 10.1002/hep.28499. Epub 2016 Mar 31.
• [10] Biologically active neutrophil chemokine pattern in tonsillitis.Clin Exp Immunol. 2004 Mar;135(3):511-8. doi: 10.1111/j.1365-2249.2003.02390.x.