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

General Information of Drug (ID: DMP9TKE)

Drug Name

PTC299 Drug Info

Synonyms

6-(4-Fluorophenyl)-2,3-dihydro-5-(4-pyridinyl)imidazo(2,1-b)thiazole; skf-86002; 72873-74-6; Skf 86002; F 86002; F 86002-A(2); UNII-9R6QDF1UO7; 9R6QDF1UO7; CHEMBL313417; 5-(4-Pyridyl)-6-(4-fluorophenyl)-2,3-dihydroimidazo(2,1-b)-thiazole; 4-[6-(4-fluorophenyl)-2H,3H-imidazo[2,1-b][1,3]thiazol-5-yl]pyridine; 6-(4-fluorophenyl)-5-(4-pyridyl)-2,3-dihydroimidazo[2,1-b]thiazole; 6-(4-Fluorophenyl)-2,3-dihydro-5-(4-pyridyl)imidazo[2,1-b]thiazole; Imidazo(2,1-b)thiazole,; SK&F 86002

Indication

Disease Entry	ICD 11	Status	REF
Rheumatoid arthritis	FA20	Phase 2	[1]
Solid tumour/cancer	2A00-2F9Z	Phase 2	[2]

Therapeutic Class

Anticancer Agents

Cross-matching ID

PubChem CID: 49787172
TTD Drug ID: DMP9TKE

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Arachidonate 5-lipoxygenase (5-LOX)	TT2J34L	LOX5_HUMAN	Inhibitor	[3]
Vascular endothelial growth factor A (VEGFA)	TTOHSBA	VEGFA_HUMAN	Modulator	[4]

------------------------------------------------------------------------------------

The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule	Molecule Type	Gene Name	Liver	Colon	Kidney	Small Intestine
Vascular endothelial growth factor A (VEGFA)	DTT	VEGFA	8.544	6.927	7.253	7.839
Arachidonate 5-lipoxygenase (5-LOX)	DTT	ALOX5	4.966	5.133	5.358	6.128

Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

The Studied Disease

Rheumatoid arthritis

ICD Disease Classification

FA20

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Vascular endothelial growth factor A (VEGFA)	DTT	VEGFA	3.61E-01	0.15	0.47

Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1	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. (Ligand id: 6040).
2	ClinicalTrials.gov (NCT00911248) PTC299 for Treatment of Neurofibromatosis Type 2. U.S. National Institutes of Health.
3	Therapeutic intervention in a rat model of ARDS: I. Dual inhibition of arachidonic acid metabolism. Circ Shock. 1990 Nov;32(3):231-42.
4	Phase I and pharmacokinetic trial of PTC299 in pediatric patients with refractory or recurrent central nervous system tumors: a PBTC study.J Neurooncol.2015 Jan;121(1):217-24.