NAV

Ripretinib

Targets (6)Enzymes (6)Carriers (2)Transporters (3)

Identification

Name
Ripretinib
Accession Number
DB14840
Description

Ripretinib is a kinase inhibitor used for the treatment of advanced gastrointestinal stromal tumor (GIST) that has not adequately responded to other kinase inhibitors such as sunitinib and imatinib. Ripretinib, also known as Qinlock, is manufactured by Deciphera Pharmaceuticals and was initially approved by the FDA on May 15, 2020.7

It is the first drug approved as a fourth-line therapy in the specific setting of prior treatment with a minimum of 3 other kinase inhibitors.8

Type
Small Molecule
Groups
Approved
Structure
Thumb
3D
Similar Structures
Weight
Average: 510.367
Monoisotopic: 509.086266
Chemical Formula
C24H21BrFN5O2
Synonyms
  • Ripretinib
External IDs
  • DCC-2618

Pharmacology

Indication

Ripretinib is indicated to treat adults diagnosed with advanced gastrointestinal stromal tumor (GIST) who have had prior therapy with at least 3 kinase inhibitors, including the imatinib.7

Associated Conditions
Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
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Pharmacodynamics

As a broad-spectrum kinase inhibitor, ripretinib inhibits various gene mutations, increasing progression-free survival in patients with advanced gastrointestinal stromal tumors (GIST).10,11 It is effective in treating mutations that are resistant to chemotherapy with other kinase inhibitors, such as imatinib.7

Ripretinib has the propensity to cause cardiac dysfunction and new primary cutaneous malignancy. It is important to measure cardiac ejection fraction before and during treatment as well as to perform regular dermatological assessments.7

Mechanism of action

Protein kinases play important roles in cellular function, and their dysregulation can lead to carcinogenesis.4 Ripretinib inhibits protein kinases including wild type and mutant platelet-derived growth factor receptor A (PDGFRA) and KIT that cause the majority of gastrointestinal stromal tumor (GIST).5 In vitro, ripretinib has been shown to inhibit PDGFRB, BRAF, VEGF, and TIE2 genes.2,3,7

Ripretinib binds to KIT and PDGFRA receptors with mutations on the exons 9, 11, 13, 14, 17 and 18 (for KIT mutations), and exons 12, 14 and 18 (for PDGFRA mutations).1 The “switch pocket” of a protein kinase is normally bound to the activation loop, acting as an “on-off switch” of a kinase. Ripretinib boasts a unique dual mechanism of action of binding to the kinase switch pocket as well as the activation loop, thereby turning off the kinase and its ability to cause dysregulated cell growth.1,9

TargetActionsOrganism
AMast/stem cell growth factor receptor Kit
inhibitor
Humans
APlatelet-derived growth factor receptor beta
inhibitor
Humans
AAngiopoietin-1 receptor
inhibitor
Humans
AVascular endothelial growth factor receptor 2
inhibitor
Humans
ASerine/threonine-protein kinase B-raf
inhibitor
Humans
APlatelet-derived growth factor receptor alpha
inhibitor
Humans
Absorption

Ripretinib is absorbed in the gastrointestinal tract and Tmax is achieved in 4 hours, with steady-state concentrations reached within 14 days.7

Volume of distribution

The mean volume of distribution of ripretinib is 307 L.7

Protein binding

Ripretinib is over 99% bound to albumin and alpha-1 acid glycoprotein. 7

Metabolism

Ripretinib is metabolized by the CYP3A subfamily of enzymes with contributions from CYP2D6 and CYP2E1 to its active metabolite, DP-5439.7

Hover over products below to view reaction partners

Route of elimination

Ripretinib is 34% excreted in the feces and 0.2% excreted in the urine.7

Half-life

The average half-life of ripretinib is 14.8 hours.7

Clearance

The mean apparent clearance of ripretinib is 15.3 L/hour.7

Adverse Effects
Learn about our commercial Adverse Effects data.
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Toxicity

There is limited information in the literature regarding an overdose with ripretinib, and LD50 information is not readily available.7 Like other kinase inhibitors, an overdose with ripretinib likely results in hematological toxicity, skin toxicity, as well as muscle, liver, and gastrointestinal toxicity.6,7

Affected organisms
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
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AbametapirThe serum concentration of Ripretinib can be increased when it is combined with Abametapir.
AbemaciclibThe serum concentration of Ripretinib can be increased when it is combined with Abemaciclib.
AcyclovirThe excretion of Acyclovir can be decreased when combined with Ripretinib.
AfatinibThe serum concentration of Ripretinib can be increased when it is combined with Afatinib.
AlectinibAlectinib may decrease the excretion rate of Ripretinib which could result in a higher serum level.
AllopurinolRipretinib may decrease the excretion rate of Allopurinol which could result in a higher serum level.
AlpelisibThe serum concentration of Alpelisib can be increased when it is combined with Ripretinib.
AmbrisentanThe serum concentration of Ambrisentan can be increased when it is combined with Ripretinib.
AmiodaroneThe serum concentration of Ripretinib can be increased when it is combined with Amiodarone.
ApalutamideThe serum concentration of Ripretinib can be decreased when it is combined with Apalutamide.
Additional Data Available
  • Extended Description
    Extended Description
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    Extended description of the mechanism of action and particular properties of each drug interaction.

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  • Severity
    Severity
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    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level
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    A rating for the strength of the evidence supporting each drug interaction.

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  • Action
    Action
    Available for Purchase

    An effect category for each drug interaction. Know how this interaction affects the subject drug.

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Food Interactions
  • Take with or without food.

Products

Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Unlock Additional Data
QinlockTablet50 mgOralDeciphera Pharmaceuticals. LlcNot applicableNot applicableCanada flag
QinlockTablet50 mg/1OralDeciphera Pharmaceuticals, LLC2020-05-15Not applicableUS flag
Additional Data Available
  • Application Number
    Application Number
    Available for Purchase

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code
    Available for Purchase

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Categories

Drug Categories
Classification
Not classified

Chemical Identifiers

UNII
9XW757O13D
CAS number
1442472-39-0
InChI Key
CEFJVGZHQAGLHS-UHFFFAOYSA-N
InChI
InChI=1S/C24H21BrFN5O2/c1-3-31-21-12-22(27-2)28-13-14(21)9-17(23(31)32)16-10-20(19(26)11-18(16)25)30-24(33)29-15-7-5-4-6-8-15/h4-13H,3H2,1-2H3,(H,27,28)(H2,29,30,33)
IUPAC Name
1-{4-bromo-5-[1-ethyl-7-(methylamino)-2-oxo-1,2-dihydro-1,6-naphthyridin-3-yl]-2-fluorophenyl}-3-phenylurea
SMILES
CCN1C(=O)C(=CC2=C1C=C(NC)N=C2)C1=C(Br)C=C(F)C(NC(=O)NC2=CC=CC=C2)=C1

References

General References
  1. Nemunaitis J, Bauer S, Blay JY, Choucair K, Gelderblom H, George S, Schoffski P, Mehren MV, Zalcberg J, Achour H, Ruiz-Soto R, Heinrich MC: Intrigue: Phase III study of ripretinib versus sunitinib in advanced gastrointestinal stromal tumor after imatinib. Future Oncol. 2020 Jan;16(1):4251-4264. doi: 10.2217/fon-2019-0633. Epub 2019 Nov 22. [PubMed:31755321]
  2. Mazzocca A, Napolitano A, Silletta M, Spalato Ceruso M, Santini D, Tonini G, Vincenzi B: New frontiers in the medical management of gastrointestinal stromal tumours. Ther Adv Med Oncol. 2019 May 17;11:1758835919841946. doi: 10.1177/1758835919841946. eCollection 2019. [PubMed:31205499]
  3. Villanueva MT: Ripretinib turns off the switch in GIST. Nat Rev Drug Discov. 2019 Jul;18(7):499. doi: 10.1038/d41573-019-00099-4. [PubMed:31267077]
  4. Kannaiyan R, Mahadevan D: A comprehensive review of protein kinase inhibitors for cancer therapy. Expert Rev Anticancer Ther. 2018 Dec;18(12):1249-1270. doi: 10.1080/14737140.2018.1527688. Epub 2018 Oct 9. [PubMed:30259761]
  5. Liu P, Tan F, Liu H, Li B, Lei T, Zhao X: The Use of Molecular Subtypes for Precision Therapy of Recurrent and Metastatic Gastrointestinal Stromal Tumor. Onco Targets Ther. 2020 Mar 24;13:2433-2447. doi: 10.2147/OTT.S241331. eCollection 2020. [PubMed:32273716]
  6. Kozuki T: Skin problems and EGFR-tyrosine kinase inhibitor. Jpn J Clin Oncol. 2016 Apr;46(4):291-8. doi: 10.1093/jjco/hyv207. Epub 2016 Jan 29. [PubMed:26826719]
  7. FDA Approved Drug Products: QINLOCK (ripretinib) tablets, for oral use [Link]
  8. FDA Approves First Drug for Fourth-Line Treatment of Advanced Gastrointestinal Stromal Tumors [Link]
  9. GIST Support International: Switch Pocket Kinase Inhibitors [Link]
  10. Deciphera phase 1 study results [Link]
  11. Deciphera phase 3 study results [Link]
ChemSpider
67886378
RxNav
2369389
ChEMBL
CHEMBL4216467
Wikipedia
Ripretinib
FDA label
Download (817 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
3Active Not RecruitingTreatmentGastrointestinal Stromal Tumors2
2Active Not RecruitingTreatmentGastrointestinal Stromal Tumors1
2RecruitingTreatmentGastrointestinal Stromal Tumor(GIST)1
1Not Yet RecruitingTreatmentGIST - Gastrointestinal Stromal Tumor1
1RecruitingTreatmentAdvanced Cancers / Advanced Systemic Mastocytosis / Gastrointestinal Stromal Tumors1
Not AvailableApproved for MarketingNot AvailableGIST - Gastrointestinal Stromal Tumor1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
TabletOral50 mg
TabletOral50 mg/1
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
Unlock Additional Data
US8940756No2012-06-072032-06-07US flag
US8461179No2012-06-072032-06-07US flag
US8188113No2010-07-272030-07-27US flag
Additional Data Available
  • Filed On
    Filed On
    Available for Purchase

    The date on which a patent was filed with the relevant government.

    Learn more

Properties

State
Solid
Experimental Properties
PropertyValueSource
boiling point (°C)568.6±50.0http://www.chemspider.com/Chemical-Structure.67886378.html
logP5.63https://www.chemsrc.com/en/cas/1225278-16-9_525350.html
pKa12.10https://www.chemicalbook.com/ChemicalProductProperty_EN_CB62627748.htm
Predicted Properties
PropertyValueSource
Water Solubility0.00583 mg/mLALOGPS
logP4.3ALOGPS
logP4.39ChemAxon
logS-4.9ALOGPS
pKa (Strongest Acidic)10.34ChemAxon
pKa (Strongest Basic)5.85ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area86.36 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity133.78 m3·mol-1ChemAxon
Polarizability47.21 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Targets

Details1. Mast/stem cell growth factor receptor Kit
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
Transmembrane receptor protein tyrosine kinase activity
Specific Function
Tyrosine-protein kinase that acts as cell-surface receptor for the cytokine KITLG/SCF and plays an essential role in the regulation of cell survival and proliferation, hematopoiesis, stem cell main...
Gene Name
KIT
Uniprot ID
P10721
Uniprot Name
Mast/stem cell growth factor receptor Kit
Molecular Weight
109863.655 Da
References
  1. Nemunaitis J, Bauer S, Blay JY, Choucair K, Gelderblom H, George S, Schoffski P, Mehren MV, Zalcberg J, Achour H, Ruiz-Soto R, Heinrich MC: Intrigue: Phase III study of ripretinib versus sunitinib in advanced gastrointestinal stromal tumor after imatinib. Future Oncol. 2020 Jan;16(1):4251-4264. doi: 10.2217/fon-2019-0633. Epub 2019 Nov 22. [PubMed:31755321]
  2. Liu P, Tan F, Liu H, Li B, Lei T, Zhao X: The Use of Molecular Subtypes for Precision Therapy of Recurrent and Metastatic Gastrointestinal Stromal Tumor. Onco Targets Ther. 2020 Mar 24;13:2433-2447. doi: 10.2147/OTT.S241331. eCollection 2020. [PubMed:32273716]
  3. FDA Approved Drug Products: QINLOCK (ripretinib) tablets, for oral use [Link]
Details2. Platelet-derived growth factor receptor beta
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
Curator comments
Supported by in vitro studies only.
General Function
Vascular endothelial growth factor binding
Specific Function
Tyrosine-protein kinase that acts as cell-surface receptor for homodimeric PDGFB and PDGFD and for heterodimers formed by PDGFA and PDGFB, and plays an essential role in the regulation of embryonic...
Gene Name
PDGFRB
Uniprot ID
P09619
Uniprot Name
Platelet-derived growth factor receptor beta
Molecular Weight
123966.895 Da
References
  1. Nemunaitis J, Bauer S, Blay JY, Choucair K, Gelderblom H, George S, Schoffski P, Mehren MV, Zalcberg J, Achour H, Ruiz-Soto R, Heinrich MC: Intrigue: Phase III study of ripretinib versus sunitinib in advanced gastrointestinal stromal tumor after imatinib. Future Oncol. 2020 Jan;16(1):4251-4264. doi: 10.2217/fon-2019-0633. Epub 2019 Nov 22. [PubMed:31755321]
  2. FDA Approved Drug Products: QINLOCK (ripretinib) tablets, for oral use [Link]
Details3. Angiopoietin-1 receptor
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
Curator comments
Supported by Supported by in vitro studies only.
General Function
Transmembrane receptor protein tyrosine kinase activity
Specific Function
Tyrosine-protein kinase that acts as cell-surface receptor for ANGPT1, ANGPT2 and ANGPT4 and regulates angiogenesis, endothelial cell survival, proliferation, migration, adhesion and cell spreading...
Gene Name
TEK
Uniprot ID
Q02763
Uniprot Name
Angiopoietin-1 receptor
Molecular Weight
125829.005 Da
References
  1. FDA Approved Drug Products: QINLOCK (ripretinib) tablets, for oral use [Link]
Details4. Vascular endothelial growth factor receptor 2
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
Curator comments
Supported by in vitro studies only.
General Function
Vascular endothelial growth factor-activated receptor activity
Specific Function
Tyrosine-protein kinase that acts as a cell-surface receptor for VEGFA, VEGFC and VEGFD. Plays an essential role in the regulation of angiogenesis, vascular development, vascular permeability, and ...
Gene Name
KDR
Uniprot ID
P35968
Uniprot Name
Vascular endothelial growth factor receptor 2
Molecular Weight
151525.555 Da
References
  1. FDA Approved Drug Products: QINLOCK (ripretinib) tablets, for oral use [Link]
Details5. Serine/threonine-protein kinase B-raf
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
Curator comments
Supported by in vitro studies only.
General Function
Protein serine/threonine kinase activity
Specific Function
Protein kinase involved in the transduction of mitogenic signals from the cell membrane to the nucleus. May play a role in the postsynaptic responses of hippocampal neuron. Phosphorylates MAP2K1, a...
Gene Name
BRAF
Uniprot ID
P15056
Uniprot Name
Serine/threonine-protein kinase B-raf
Molecular Weight
84436.135 Da
References
  1. FDA Approved Drug Products: QINLOCK (ripretinib) tablets, for oral use [Link]
Details6. Platelet-derived growth factor receptor alpha
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
Vascular endothelial growth factor-activated receptor activity
Specific Function
Tyrosine-protein kinase that acts as a cell-surface receptor for PDGFA, PDGFB and PDGFC and plays an essential role in the regulation of embryonic development, cell proliferation, survival and chem...
Gene Name
PDGFRA
Uniprot ID
P16234
Uniprot Name
Platelet-derived growth factor receptor alpha
Molecular Weight
122668.46 Da
References
  1. Villanueva MT: Ripretinib turns off the switch in GIST. Nat Rev Drug Discov. 2019 Jul;18(7):499. doi: 10.1038/d41573-019-00099-4. [PubMed:31267077]
  2. Mazzocca A, Napolitano A, Silletta M, Spalato Ceruso M, Santini D, Tonini G, Vincenzi B: New frontiers in the medical management of gastrointestinal stromal tumours. Ther Adv Med Oncol. 2019 May 17;11:1758835919841946. doi: 10.1177/1758835919841946. eCollection 2019. [PubMed:31205499]
  3. FDA Approved Drug Products: QINLOCK (ripretinib) tablets, for oral use [Link]

Enzymes

Details1. Cytochrome P450 2C8
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Inhibitor
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2C8
Uniprot ID
P10632
Uniprot Name
Cytochrome P450 2C8
Molecular Weight
55824.275 Da
References
  1. FDA Approved Drug Products: QINLOCK (ripretinib) tablets, for oral use [Link]
Details2. Mast/stem cell growth factor receptor Kit
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
Transmembrane receptor protein tyrosine kinase activity
Specific Function
Tyrosine-protein kinase that acts as cell-surface receptor for the cytokine KITLG/SCF and plays an essential role in the regulation of cell survival and proliferation, hematopoiesis, stem cell main...
Gene Name
KIT
Uniprot ID
P10721
Uniprot Name
Mast/stem cell growth factor receptor Kit
Molecular Weight
109863.655 Da
References
  1. Nemunaitis J, Bauer S, Blay JY, Choucair K, Gelderblom H, George S, Schoffski P, Mehren MV, Zalcberg J, Achour H, Ruiz-Soto R, Heinrich MC: Intrigue: Phase III study of ripretinib versus sunitinib in advanced gastrointestinal stromal tumor after imatinib. Future Oncol. 2020 Jan;16(1):4251-4264. doi: 10.2217/fon-2019-0633. Epub 2019 Nov 22. [PubMed:31755321]
  2. Liu P, Tan F, Liu H, Li B, Lei T, Zhao X: The Use of Molecular Subtypes for Precision Therapy of Recurrent and Metastatic Gastrointestinal Stromal Tumor. Onco Targets Ther. 2020 Mar 24;13:2433-2447. doi: 10.2147/OTT.S241331. eCollection 2020. [PubMed:32273716]
  3. FDA Approved Drug Products: QINLOCK (ripretinib) tablets, for oral use [Link]
Details3. Platelet-derived growth factor receptor alpha
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Vascular endothelial growth factor-activated receptor activity
Specific Function
Tyrosine-protein kinase that acts as a cell-surface receptor for PDGFA, PDGFB and PDGFC and plays an essential role in the regulation of embryonic development, cell proliferation, survival and chem...
Gene Name
PDGFRA
Uniprot ID
P16234
Uniprot Name
Platelet-derived growth factor receptor alpha
Molecular Weight
122668.46 Da
References
  1. Nemunaitis J, Bauer S, Blay JY, Choucair K, Gelderblom H, George S, Schoffski P, Mehren MV, Zalcberg J, Achour H, Ruiz-Soto R, Heinrich MC: Intrigue: Phase III study of ripretinib versus sunitinib in advanced gastrointestinal stromal tumor after imatinib. Future Oncol. 2020 Jan;16(1):4251-4264. doi: 10.2217/fon-2019-0633. Epub 2019 Nov 22. [PubMed:31755321]
  2. Liu P, Tan F, Liu H, Li B, Lei T, Zhao X: The Use of Molecular Subtypes for Precision Therapy of Recurrent and Metastatic Gastrointestinal Stromal Tumor. Onco Targets Ther. 2020 Mar 24;13:2433-2447. doi: 10.2147/OTT.S241331. eCollection 2020. [PubMed:32273716]
  3. FDA Approved Drug Products: QINLOCK (ripretinib) tablets, for oral use [Link]
Details4. Cytochrome P450 3A4
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. FDA Approved Drug Products: QINLOCK (ripretinib) tablets, for oral use [Link]
Details5. Cytochrome P450 2D6
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 Da
References
  1. FDA Approved Drug Products: QINLOCK (ripretinib) tablets, for oral use [Link]
Details6. Cytochrome P450 2E1
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Steroid hydroxylase activity
Specific Function
Metabolizes several precarcinogens, drugs, and solvents to reactive metabolites. Inactivates a number of drugs and xenobiotics and also bioactivates many xenobiotic substrates to their hepatotoxic ...
Gene Name
CYP2E1
Uniprot ID
P05181
Uniprot Name
Cytochrome P450 2E1
Molecular Weight
56848.42 Da
References
  1. FDA Approved Drug Products: QINLOCK (ripretinib) tablets, for oral use [Link]

Carriers

Details1. Serum albumin
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
General Function
Toxic substance binding
Specific Function
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
Gene Name
ALB
Uniprot ID
P02768
Uniprot Name
Serum albumin
Molecular Weight
69365.94 Da
References
  1. FDA Approved Drug Products: QINLOCK (ripretinib) tablets, for oral use [Link]
Details2. alpha1-acid glycoprotein (Protein Group)
Kind
Protein group
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
General Function
Not Available
Specific Function
Functions as transport protein in the blood stream. Binds various ligands in the interior of its beta-barrel domain. Also binds synthetic drugs and influences their distribution and availability in...
Components:
NameUniProt ID
Alpha-1-acid glycoprotein 1P02763
Alpha-1-acid glycoprotein 2P19652
References
  1. FDA Approved Drug Products: QINLOCK (ripretinib) tablets, for oral use [Link]

Transporters

Details1. P-glycoprotein 1
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. FDA Approved Drug Products: QINLOCK (ripretinib) tablets, for oral use [Link]
Details2. ATP-binding cassette sub-family G member 2
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Xenobiotic-transporting atpase activity
Specific Function
High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both fro...
Gene Name
ABCG2
Uniprot ID
Q9UNQ0
Uniprot Name
ATP-binding cassette sub-family G member 2
Molecular Weight
72313.47 Da
References
  1. FDA Approved Drug Products: QINLOCK (ripretinib) tablets, for oral use [Link]
Details3. Multidrug and toxin extrusion protein 1
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Monovalent cation:proton antiporter activity
Specific Function
Solute transporter for tetraethylammonium (TEA), 1-methyl-4-phenylpyridinium (MPP), cimetidine, N-methylnicotinamide (NMN), metformin, creatinine, guanidine, procainamide, topotecan, estrone sulfat...
Gene Name
SLC47A1
Uniprot ID
Q96FL8
Uniprot Name
Multidrug and toxin extrusion protein 1
Molecular Weight
61921.585 Da
References
  1. FDA Approved Drug Products: QINLOCK (ripretinib) tablets, for oral use [Link]

Drug created on May 20, 2019 08:29 / Updated on December 02, 2020 08:59