Identification
- Summary
Ripretinib is a kinase inhibitor used to treat advanced gastrointestinal stromal tumor (GIST).
- Brand Names
- Qinlock
- Generic Name
- Ripretinib
- DrugBank Accession Number
- DB14840
- Background
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
Structure for Ripretinib (DB14840)
- 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 with imatinib.7
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- Contraindications & Blackbox Warnings
Avoid life-threatening adverse drug eventsImprove clinical decision support with information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events & improve clinical decision support.- 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
Target Actions Organism AMast/stem cell growth factor receptor Kit inhibitorHumans APlatelet-derived growth factor receptor beta inhibitorHumans AAngiopoietin-1 receptor inhibitorHumans AVascular endothelial growth factor receptor 2 inhibitorHumans ASerine/threonine-protein kinase B-raf inhibitorHumans APlatelet-derived growth factor receptor alpha inhibitorHumans - 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
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- 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
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates.Improve decision support & research outcomes with our structured adverse effects data.- 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
- 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.
Drug Interaction Integrate drug-drug
interactions in your softwareAbametapir The serum concentration of Ripretinib can be increased when it is combined with Abametapir. Abemaciclib The serum concentration of Abemaciclib can be increased when it is combined with Ripretinib. Abrocitinib The serum concentration of Ripretinib can be increased when it is combined with Abrocitinib. Acyclovir The excretion of Acyclovir can be decreased when combined with Ripretinib. Afatinib The serum concentration of Afatinib can be increased when it is combined with Ripretinib. Alectinib Alectinib may decrease the excretion rate of Ripretinib which could result in a higher serum level. Allopurinol Ripretinib may decrease the excretion rate of Allopurinol which could result in a higher serum level. Alpelisib The serum concentration of Alpelisib can be increased when it is combined with Ripretinib. Ambrisentan The serum concentration of Ambrisentan can be increased when it is combined with Ripretinib. Amiodarone The serum concentration of Ripretinib can be increased when it is combined with Amiodarone. 
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- Take with or without food.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Qinlock Tablet 50 mg Oral Deciphera Pharmaceuticals. Llc 2020-12-10 Not applicable Canada 
Qinlock Tablet 50 mg Oral Deciphera Pharmaceuticals (Netherlands) B.V. 2022-01-18 Not applicable EU 
Qinlock Tablet 50 mg/1 Oral Deciphera Pharmaceuticals, LLC 2020-05-15 Not applicable US 
Qinlock Tablet 50 mg Oral Deciphera Pharmaceuticals (Netherlands) B.V. 2022-01-18 Not applicable EU
Categories
- ATC Codes
- L01EX19 — Ripretinib
- Drug Categories
- Amides
- Antineoplastic Agents
- Antineoplastic and Immunomodulating Agents
- BCRP/ABCG2 Inhibitors
- BCRP/ABCG2 Substrates
- Cytochrome P-450 CYP2C8 Inhibitors
- Cytochrome P-450 CYP2C8 Inhibitors (strength unknown)
- Cytochrome P-450 CYP2D6 Substrates
- Cytochrome P-450 CYP2E1 Substrates
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 Enzyme Inhibitors
- Cytochrome P-450 Substrates
- Heterocyclic Compounds, Fused-Ring
- Kinase Inhibitor
- MATE 1 Inhibitors
- MATE inhibitors
- P-glycoprotein inhibitors
- P-glycoprotein substrates
- Platelet-derived Growth Factor alpha Receptor Inhibitors
- Protein Kinase Inhibitors
- Stem Cell Factor (KIT) Receptor Inhibitors
- Classification
- Not classified
- Affected organisms
- Not Available
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
- 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. [Article]
- 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. [Article]
- 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. [Article]
- 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. [Article]
- 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. [Article]
- 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. [Article]
- FDA Approved Drug Products: Qinlock (ripretinib) tablets for oral use [Link]
- FDA Approves First Drug for Fourth-Line Treatment of Advanced Gastrointestinal Stromal Tumors [Link]
- GIST Support International: Switch Pocket Kinase Inhibitors [Link]
- Deciphera phase 1 study results [Link]
- Deciphera phase 3 study results [Link]
- External Links
- Human Metabolome Database
- HMDB0304864
- ChemSpider
- 67886378
- 2369389
- ChEMBL
- CHEMBL4216467
- PharmGKB
- PA166270781
- Wikipedia
- Ripretinib
- FDA label
- Download (817 KB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 3 Active Not Recruiting Treatment Gastrointestinal Stromal Tumor (GIST) 1 3 Completed Treatment Gastrointestinal Stromal Tumor (GIST) 1 2 Completed Treatment Gastrointestinal Stromal Tumor (GIST) 2 1 Completed Treatment Advanced Malignant Neoplasm / Advanced Systemic Mastocytosis (AdvSM) / Gastrointestinal Stromal Tumor (GIST) 1 1 Recruiting Treatment Gastrointestinal Stromal Tumor (GIST) 1 1, 2 Withdrawn Treatment Gastrointestinal Stromal Tumor (GIST) 1 Not Available Active Not Recruiting Not Available Gastrointestinal Stromal Tumor (GIST) 1 Not Available Approved for Marketing Not Available Gastrointestinal Stromal Tumor (GIST) 1 Not Available Recruiting Treatment Gastrointestinal Stromal Tumor (GIST) 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Tablet Oral 50 mg Tablet Oral 50 mg/1 - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US8940756 No 2015-01-27 2032-06-07 US US8461179 No 2013-06-11 2032-06-07 US US8188113 No 2012-05-29 2030-07-27 US US10966966 No 2021-04-06 2040-08-12 US USRE48731 No 2021-09-14 2032-06-07 US US11185535 No 2021-11-30 2040-12-30 US US11266635 No 2020-08-12 2040-08-12 US US11344536 No 2020-08-12 2040-08-12 US US11395818 No 2020-12-30 2040-12-30 US US11426390 No 2020-08-12 2040-08-12 US US11433056 No 2020-08-12 2040-08-12 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source boiling point (°C) 568.6±50.0 http://www.chemspider.com/Chemical-Structure.67886378.html logP 5.63 https://www.chemsrc.com/en/cas/1225278-16-9_525350.html pKa 12.10 https://www.chemicalbook.com/ChemicalProductProperty_EN_CB62627748.htm - Predicted Properties
Property Value Source Water Solubility 0.00583 mg/mL ALOGPS logP 4.3 ALOGPS logP 4.39 Chemaxon logS -4.9 ALOGPS pKa (Strongest Acidic) 10.34 Chemaxon pKa (Strongest Basic) 5.85 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 4 Chemaxon Hydrogen Donor Count 3 Chemaxon Polar Surface Area 86.36 Å2 Chemaxon Rotatable Bond Count 5 Chemaxon Refractivity 133.78 m3·mol-1 Chemaxon Polarizability 47.21 Å3 Chemaxon Number of Rings 4 Chemaxon Bioavailability 1 Chemaxon Rule of Five No Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Not Available
Targets
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- 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
- 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. [Article]
- 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. [Article]
- FDA Approved Drug Products: Qinlock (ripretinib) tablets for oral use [Link]
- 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
- 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. [Article]
- FDA Approved Drug Products: Qinlock (ripretinib) tablets for oral use [Link]
- 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
- FDA Approved Drug Products: Qinlock (ripretinib) tablets for oral use [Link]
- 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
- FDA Approved Drug Products: Qinlock (ripretinib) tablets for oral use [Link]
- 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
- FDA Approved Drug Products: Qinlock (ripretinib) tablets for oral use [Link]
- 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
- 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. [Article]
- 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. [Article]
- FDA Approved Drug Products: Qinlock (ripretinib) tablets for oral use [Link]
Enzymes
- 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
- FDA Approved Drug Products: Qinlock (ripretinib) tablets for oral use [Link]
- 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
- 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. [Article]
- 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. [Article]
- FDA Approved Drug Products: Qinlock (ripretinib) tablets for oral use [Link]
- 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
- FDA Approved Drug Products: Qinlock (ripretinib) tablets for oral use [Link]
- 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
- FDA Approved Drug Products: Qinlock (ripretinib) tablets for oral use [Link]
- 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
- FDA Approved Drug Products: Qinlock (ripretinib) tablets for oral use [Link]
Carriers
- 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
- FDA Approved Drug Products: Qinlock (ripretinib) tablets for oral use [Link]
- 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:
References
- FDA Approved Drug Products: Qinlock (ripretinib) tablets for oral use [Link]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- 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
- FDA Approved Drug Products: Qinlock (ripretinib) tablets for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- 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
- FDA Approved Drug Products: Qinlock (ripretinib) tablets for oral use [Link]
- 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
- FDA Approved Drug Products: Qinlock (ripretinib) tablets for oral use [Link]
Drug created at May 20, 2019 14:29 / Updated at February 05, 2023 22:13