Target Information

Target General Information

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Target ID

T52624 (Former ID: TTDS00261)

Target Name

Platelet-derived growth factor receptor (PDGFR)

Synonyms

Platelet-derived growth factor receptor tyrosine kinase; PDGFR kinase; PDGF-R

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Gene Name

NO-GeName

Target Type

Successful target

[1]

Disease

[+] 8 Target-related Diseases

Colorectal cancer [ICD-11: 2B91]

Diabetic foot ulcer [ICD-11: BD54]

Idiopathic interstitial pneumonitis [ICD-11: CB03]

Mature B-cell lymphoma [ICD-11: 2A85]

Myeloproliferative neoplasm [ICD-11: 2A20]

Renal cell carcinoma [ICD-11: 2C90]

Coronary atherosclerosis [ICD-11: BA80]

Myocardial infarction [ICD-11: BA41-BA43]

UniProt ID

NOUNIPROTAC

Drugs and Modes of Action

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Approved Drug(s)

[+] 5 Approved Drugs

CT-102

Drug Info

Approved

Diabetic foot ulcer

[2]

Imatinib

Drug Info

Approved

Chronic myelogenous leukaemia

[3], [4]

Intedanib

Drug Info

Approved

Colorectal cancer

[5]

Pazopanib HCl

Drug Info

Approved

Renal cell carcinoma

[6]

Trapidil

Drug Info

Phase 4

Coronary artery disease

[7]

Clinical Trial Drug(s)

[+] 5 Clinical Trial Drugs

Rosiglitazone + metformin

Drug Info

Phase 3

Diabetic complication

[8]

TKI258

Drug Info

Phase 3

Renal cell carcinoma

[9]

BAY-57-9352

Drug Info

Phase 2

Solid tumour/cancer

[10]

Vorolanib

Drug Info

Phase 2

Non-small-cell lung cancer

[11]

X-82

Drug Info

Phase 2

Age-related macular degeneration

[12]

Patented Agent(s)

[+] 2 Patented Agents

PMID25623274-Compound-WO2014132220C1

Drug Info

Patented

Pulmonary arterial hypertension

[13]

PMID25623274-Compound-WO2014132220C2

Drug Info

Patented

Pulmonary arterial hypertension

[13]

Discontinued Drug(s)

[+] 2 Discontinued Drugs

Motesanib

Drug Info

Discontinued in Phase 3

Non-small-cell lung cancer

[14], [15]

CGP-53716

Drug Info

Terminated

Solid tumour/cancer

[16]

Mode of Action

[+] 3 Modes of Action

Activator

[+] 2 Activator drugs

CT-102

Drug Info

[2]

PDGF gene therapy

Drug Info

[2]

Inhibitor

[+] 10 Inhibitor drugs

Imatinib

Drug Info

[1]

Pazopanib HCl

Drug Info

[6]

Trapidil

Drug Info

[17]

Rosiglitazone + metformin

Drug Info

[1], [18]

TKI258

Drug Info

[1]

BAY-57-9352

Drug Info

[1]

Vorolanib

Drug Info

[19]

PMID25623274-Compound-WO2014132220C1

Drug Info

[13]

PMID25623274-Compound-WO2014132220C2

Drug Info

[13]

Motesanib

Drug Info

[21], [22], [23]

Modulator

[+] 3 Modulator drugs

Intedanib

Drug Info

[5]

X-82

Drug Info

[20]

CGP-53716

Drug Info

[24], [25], [26]

Chemical Structure based Activity Landscape of Target

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Drug Property Profile of Target

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(1) Molecular Weight (mw) based Drug Clustering

(2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering

(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering

(4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering

(5) Rotatable Bond Count (rotbonds) based Drug Clustering

(6) Topological Polar Surface Area (polararea) based Drug Clustering

"RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five

Co-Targets

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Co-Targets

Co-Targets Info

Target-Related Models and Studies

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Target Validation

Target Validation Info

Target QSAR Model

References

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REF 1

A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22.

REF 2

Emerging drugs for diabetic foot ulcers. Expert Opin Emerg Drugs. 2006 Nov;11(4):709-24.

REF 3

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: 5687).

REF 4

Emerging treatments for pulmonary arterial hypertension. Expert Opin Emerg Drugs. 2006 Nov;11(4):609-19.

REF 5

2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.

REF 6

Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.

REF 7

ClinicalTrials.gov (NCT00914420) Optical Coherence Tomography (OCT) Evaluation of Re-endothelization: A Comparison of the Intrepide Stent Versus Taxus . U.S. National Institutes of Health.

REF 8

ClinicalTrials.gov (NCT00499707) Efficacy and Safety Study of Rosiglitazone/Metformin Therapy vs Rosiglitazone and Metformin in Type 2 Diabetes Subjects. U.S. National Institutes of Health.

REF 9

ClinicalTrials.gov (NCT01223027) Study of Dovitinib Versus Sorafenib in Patients With Metastatic Renal Cell Carcinoma. U.S. National Institutes of Health.

REF 10

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021605)

REF 11

ClinicalTrials.gov (NCT03848611) CM082 and JS001 in Patients With Advanced Non-Small Cell Lung Cancer (NSCLC).. U.S. National Institutes of Health.

REF 12

ClinicalTrials.gov (NCT02348359) X-82 to Treat Age-related Macular Degeneration. U.S. National Institutes of Health.

REF 13

Evaluation of WO-2014132220, selective PDGFR inhibitors for the treatment of pulmonary arterial hypertension.Expert Opin Ther Pat. 2015 Apr;25(4):493-9.

REF 14

REF 15

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800011016)

REF 16

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005535)

REF 17

Osteitis fibrosa is mediated by Platelet-Derived Growth Factor-A via a phosphoinositide 3-kinase-dependent signaling pathway in a rat model for chr... Endocrinology. 2008 Nov;149(11):5735-46.

REF 18

Dose-finding study of the multitargeted tyrosine kinase inhibitor SU6668 in patients with advanced malignancies. Clin Cancer Res. 2005 Sep 1;11(17):6240-6.

REF 19

Vorolanib, an oral VEGFR/PDGFR dual tyrosine kinase inhibitor for treatment of patients with advanced solid tumors: An open-label, phase I dose escalation and dose expansion trial. Chin J Cancer Res. 2021 Feb 28;33(1):103-114.

REF 20

National Cancer Institute Drug Dictionary (drug id 695817).

REF 21

Clinical pipeline report, company report or official report of Amgen (2009).

REF 22

Phase II study of safety and efficacy of motesanib in patients with progressive or symptomatic, advanced or metastatic medullary thyroid cancer. J Clin Oncol. 2009 Aug 10;27(23):3794-801.

REF 23

Axitinib for renal cell carcinoma. Expert Opin Investig Drugs. 2008 May;17(5):741-8.

REF 24

Inhibition of cell growth: effects of the tyrosine kinase inhibitor CGP 53716. J Pharmacol Exp Ther. 1997 Oct;283(1):402-10.

REF 25

Inhibition of platelet-derived growth factor receptor tyrosine kinase inhibits vascular smooth muscle cell migration and proliferation. FASEB J. 1997 Nov;11(13):1119-26.

REF 26

Role of platelet-derived growth factor in obliterative bronchiolitis (chronic rejection) in the rat. Am J Respir Crit Care Med. 1999 Oct;160(4):1324-32.

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