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

Identification

Generic Name
Rivoceranib
DrugBank Accession Number
DB14765
Background

Rivoceranib is under investigation in clinical trial NCT02726854 (Apatinib as Second-line Treatment of Advanced Pancreatic Cancer).

Type
Small Molecule
Groups
Investigational
Structure
Weight
Average: 397.482
Monoisotopic: 397.190260381
Chemical Formula
C24H23N5O
Synonyms
  • Apatinib
  • Rivoceranib
  • YN968D1 free base

Pharmacology

Indication

Not Available

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Contraindications & Blackbox Warnings
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Pharmacodynamics

Not Available

Mechanism of action
Not Available
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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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.
DrugInteraction
ArticaineThe risk or severity of methemoglobinemia can be increased when Rivoceranib is combined with Articaine.
BenzocaineThe risk or severity of methemoglobinemia can be increased when Rivoceranib is combined with Benzocaine.
Benzyl alcoholThe risk or severity of methemoglobinemia can be increased when Rivoceranib is combined with Benzyl alcohol.
BupivacaineThe risk or severity of methemoglobinemia can be increased when Rivoceranib is combined with Bupivacaine.
ButacaineThe risk or severity of methemoglobinemia can be increased when Rivoceranib is combined with Butacaine.
ButambenThe risk or severity of methemoglobinemia can be increased when Rivoceranib is combined with Butamben.
CapsaicinThe risk or severity of methemoglobinemia can be increased when Rivoceranib is combined with Capsaicin.
ChloroprocaineThe risk or severity of methemoglobinemia can be increased when Rivoceranib is combined with Chloroprocaine.
CinchocaineThe risk or severity of methemoglobinemia can be increased when Rivoceranib is combined with Cinchocaine.
CocaineThe risk or severity of methemoglobinemia can be increased when Rivoceranib is combined with Cocaine.
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Food Interactions
Not Available

Products

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Product Ingredients
IngredientUNIICASInChI Key
Rivoceranib mesylateTK02X14ASJ1218779-75-9Not applicable

Categories

Drug Categories
Classification
Not classified
Affected organisms
Not Available

Chemical Identifiers

UNII
5S371K6132
CAS number
811803-05-1
InChI Key
WPEWQEMJFLWMLV-UHFFFAOYSA-N
InChI
InChI=1S/C24H23N5O/c25-17-24(11-1-2-12-24)19-5-7-20(8-6-19)29-23(30)21-4-3-13-27-22(21)28-16-18-9-14-26-15-10-18/h3-10,13-15H,1-2,11-12,16H2,(H,27,28)(H,29,30)
IUPAC Name
N-[4-(1-cyanocyclopentyl)phenyl]-2-{[(pyridin-4-yl)methyl]amino}pyridine-3-carboxamide
SMILES
O=C(NC1=CC=C(C=C1)C1(CCCC1)C#N)C1=CC=CN=C1NCC1=CC=NC=C1

References

General References
Not Available
Human Metabolome Database
HMDB0248505
ChemSpider
9490441
ChEMBL
CHEMBL3186534
ZINC
ZINC000070466461
Wikipedia
Apatinib

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedTreatmentBreast Cancer / Cancer / Cervical Cancer / Esophageal Cancer / Gastric Cancer / Non-Small Cell Lung Cancer, Lung Cancer, Cancer / Ovarian Cancer1
4CompletedTreatmentDiffuse Large B-Cell Lymphoma (DLBCL) / Relapsed and Refractory1
4Not Yet RecruitingTreatmentGastric Cancer / Randomized Controlled Study1
4Not Yet RecruitingTreatmentUnresectable Hepatocellular Carcinoma (HCC)1
4Unknown StatusOtherStage IV Cancer1
4Unknown StatusTreatmentAdvanced Non-squamous Cell Non-small Cell Lung Cancer1
4Unknown StatusTreatmentGastric Cancer1
4Unknown StatusTreatmentNewly Diagnosed Peripheral T-cell Lymphoma1
4Unknown StatusTreatmentSquamous Cell Lung Cancer1
3Active Not RecruitingTreatmentDifferentiated Thyroid Cancer (DTC)1

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
PropertyValueSource
Water Solubility0.012 mg/mLALOGPS
logP3.14ALOGPS
logP4.29Chemaxon
logS-4.5ALOGPS
pKa (Strongest Acidic)15.23Chemaxon
pKa (Strongest Basic)5.41Chemaxon
Physiological Charge0Chemaxon
Hydrogen Acceptor Count5Chemaxon
Hydrogen Donor Count2Chemaxon
Polar Surface Area90.7 Å2Chemaxon
Rotatable Bond Count6Chemaxon
Refractivity119.16 m3·mol-1Chemaxon
Polarizability43.36 Å3Chemaxon
Number of Rings4Chemaxon
Bioavailability1Chemaxon
Rule of FiveYesChemaxon
Ghose FilterYesChemaxon
Veber's RuleNoChemaxon
MDDR-like RuleYesChemaxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Drug created at May 20, 2019 14:25 / Updated at December 13, 2022 10:46