Explore a selection of our essential drug information below, or:
Identification
- Generic Name
- NV-52
- DrugBank Accession Number
- DB05673
- Background
NV-52 is an investigational synthetic flavonoid thromboxane synthase (TXS) inhibitor developed for the maintenance of remission in inflammatory bowel disease.
- Type
- Small Molecule
- Groups
- Investigational
- Synonyms
- Not Available
Pharmacology
- Indication
Investigated for use/treatment in inflammatory bowel disease.
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Not Available
- Mechanism of action
NV-52 is a synthetic flavonoid derivative. It is a selective thromboxane synthase (TXS) inhibitor under development for the treatment of inflammatory bowel disease. NV-52 selectively inhibits TXS in vitro in physiological relevant concentrations, causing a reduction in thromboxane B2 of ≤ 40% in association with an increase in prostaglandin E2.
Target Actions Organism UThromboxane-A synthase Not Available Humans - 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
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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
- Humans and other mammals
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
- Howes LG, Howes JB, Huang JL, Walker C: Phase Ib single- and multiple-dose pharmacokinetic study of oral NV-52 in healthy volunteers. Drugs R D. 2008;9(3):159-66. [Article]
- Howes LG, James MJ, Florin T, Walker C: Nv-52: a novel thromboxane synthase inhibitor for the treatment of inflammatory bowel disease. Expert Opin Investig Drugs. 2007 Aug;16(8):1255-66. [Article]
- External Links
- Not Available
Clinical Trials
- Clinical Trials
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Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
- Not Available
- Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
- Not Available
- Predicted Properties
- Not Available
- Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Not Available
- Chromatographic Properties
Collision Cross Sections (CCS)
Not Available
Targets
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Catalyzes the conversion of prostaglandin H2 (PGH2) to thromboxane A2 (TXA2), a potent inducer of blood vessel constriction and platelet aggregation (PubMed:11097184, PubMed:11297515, PubMed:22735388, PubMed:24009185, PubMed:8436233, PubMed:9873013). Cleaves also PGH2 to 12-hydroxy-heptadecatrienoicacid (12-HHT) and malondialdehyde, which is known to act as a mediator of DNA damage. 12-HHT and malondialdehyde are formed stoichiometrically in the same amounts as TXA2 (PubMed:11297515, PubMed:22735388, PubMed:9873013). Additionally, displays dehydratase activity, toward (15S)-hydroperoxy-(5Z,8Z,11Z,13E)-eicosatetraenoate (15(S)-HPETE) producing 15-KETE and 15-HETE (PubMed:17459323)
- Specific Function
- 12-hydroxyheptadecatrienoic acid synthase activity
- Gene Name
- TBXAS1
- Uniprot ID
- P24557
- Uniprot Name
- Thromboxane-A synthase
- Molecular Weight
- 60517.69 Da
References
- Howes LG, James MJ, Florin T, Walker C: Nv-52: a novel thromboxane synthase inhibitor for the treatment of inflammatory bowel disease. Expert Opin Investig Drugs. 2007 Aug;16(8):1255-66. [Article]
- Howes LG, Howes JB, Huang JL, Walker C: Phase Ib single- and multiple-dose pharmacokinetic study of oral NV-52 in healthy volunteers. Drugs R D. 2008;9(3):159-66. [Article]
Drug created at November 18, 2007 18:26 / Updated at July 23, 2024 18:02