PT2977

This drug entry is a stub and has not been fully annotated. It is scheduled to be annotated soon.

Identification

Generic Name
PT2977
DrugBank Accession Number
DB15463
Background

PT2977 is an HIF-2α inhibitor. A kidney cancer treatment, it is the lead candidate drug for Peloton. Peloton was acquired by Merck & Co Inc on May 21, 2019.

Type
Small Molecule
Groups
Investigational
Synonyms
Not Available
External IDs
  • PT 2977
  • PT-2977
  • PT2977

Pharmacology

Indication

Not Available

Pharmacology
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Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics

Not Available

Mechanism of action
TargetActionsOrganism
UEndothelial PAS domain-containing protein 1Not AvailableHumans
Absorption

Not Available

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism
Not Available
Route of elimination

Not Available

Half-life

Not Available

Clearance

Not Available

Adverse Effects
Medicalerrors
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Toxicity

Not Available

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Not Available
Food Interactions
Not Available

Categories

Drug Categories
Not Available
Classification
Not classified
Affected organisms
Not Available

Chemical Identifiers

UNII
Not Available
CAS number
Not Available
InChI Key
Not Available
InChI
Not Available
IUPAC Name
Not Available
SMILES
Not Available

References

General References
Not Available
Not Available

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
3RecruitingTreatmentRenal Cell Adenocarcinoma2
2Active Not RecruitingTreatmentVHL - Von Hippel-Lindau Syndrome / VHL Gene Inactivation / VHL Gene Mutation / VHL Syndrome / VHL-Associated Clear Cell Renal Cell Carcinoma / VHL-Associated Renal Cell Carcinoma1
2RecruitingTreatmentClear Cell Renal Cell Carcinoma (ccRCC) / Kidney / Renal Cancers / Renal Cell Adenocarcinoma / Renal Cell Cancer Metastatic / Renal Cell Cancer, Recurrent / Renal Cell Carcinoma Recurrent1
2RecruitingTreatmentRenal Cell Adenocarcinoma1
1Active Not RecruitingTreatmentCcRCC / GBM / Glioblastoma Multiforme (GBM) / Glioblastoma, Adult / Glioblastomas / RCC / RCC, Clear Cell Adenocarcinoma / Renal Cancers / Renal Cell Carcinoma Recurrent / Renal Cell Carcinoma, Clear Cell / Renal Cell Carcinoma, Clear Cell Adenocarcinoma / Renal Cell Carcinoma, Metastatic / Solid Carcinoma / Solid Tumors, Adult / Solid Tumors, Advanced Solid Tumors / Tumors, Solid1
1CompletedTreatmentHealthy Volunteers1
1RecruitingTreatmentRenal Cell Adenocarcinoma1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Not Available
Experimental Properties
Not Available
Predicted Properties
Not Available
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Targets

Drugtargets
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Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Transcription factor involved in the induction of oxygen regulated genes. Heterodimerizes with ARNT; heterodimer binds to core DNA sequence 5'-TACGTG-3' within the hypoxia response element (HRE) of target gene promoters (By similarity). Regulates the vascular endothelial growth factor (VEGF) expression and seems to be implicated in the development of blood vessels and the tubular system of lung. May also play a role in the formation of the endothelium that gives rise to the blood brain barrier. Potent activator of the Tie-2 tyrosine kinase expression. Activation requires recruitment of transcriptional coactivators such as CREBBP and probably EP300. Interaction with redox regulatory protein APEX seems to activate CTAD (By similarity).
Specific Function
Dna binding
Gene Name
EPAS1
Uniprot ID
Q99814
Uniprot Name
Endothelial PAS domain-containing protein 1
Molecular Weight
96458.235 Da
References
  1. Tai W. Wong, Rajeev Shrimali, Cristina Contreras, Tzuling Cheng, Robert M. Czerwinski, Daryl D. Dixon, Xinlin Du, Craig Fett, Jessica Goree, Jonas A. Grina, Guangzhou Han, Heli Huang, Jim Rizzi, Stephen T. Schlachter, Bin Wang, Keshi Wang, Paul M. Wehn, Shanhai Xie, Rui Xu, Hanbiao Yang, John A. Josey and Eli M. Wallace: Abstract B140: PT2977, a novel HIF-2a antagonist, has potent antitumor activity and remodels the immunosuppressive tumor microenvironment in clear cell renal cell cancer AACR-NCI-EORTC International Conference: Molecular Targets and Cancer Therapeutics. [Article]

Drug created on May 21, 2019 17:13 / Updated on June 12, 2020 16:53