Identification
- Summary
Asciminib is an inhibitor of ABL/BCR-ABL1 tyrosine kinase for the treatment of patients with Philadelphia chromosome-positive CML, including those with the T315I mutation.
- Brand Names
- Scemblix
- Generic Name
- Asciminib
- DrugBank Accession Number
- DB12597
- Background
Asciminib is a tyrosine kinase inhibitor (TKI) used in the treatment of chronic-phase Philadelphia chromosome-positive chronic myeloid leukemia (Ph+ CML). More specifically, it is an inhibitor of the ABL1 kinase activity of the BCR-ABL1 fusion protein6 which serves as a driver of CML proliferation in most patients with the disease.8 It has also shown benefit in Ph+ CML with the T315I mutation, which produces a mutant BCR-ABL1 which is typically treatment-resistant as compared to wild-type BCR-ABL1.
Existing inhibitors of ABL compete at the ATP binding sites of these proteins and can be classified into those that target the active conformation of the kinase domain (dasatinib, bosutinib) and those that target the inactive kinase domain (imatinib, nilotinib, ponatinib).5 Asciminib is unique in that it acts as an allosteric inhibitor, binding at the myristoyl pocket of the BCR-ABL1 protein and locking it into an inactive conformation.6,3
Asciminib received FDA approval on October 29, 2021 (Scemblix, Novartis AG).7
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
Structure for Asciminib (DB12597)
- Weight
- Average: 449.84
Monoisotopic: 449.1066235 - Chemical Formula
- C20H18ClF2N5O3
- Synonyms
- Asciminib
- External IDs
- ABL-001
- ABL001
- ABL001-NX
- NVP-ABL001
Pharmacology
- Indication
Asciminib is indicated for the treatment of adult patients with Philadelphia chromosome-positive chronic myeloid leukemia (Ph+ CML) in chronic phase who have been previously treated with ≥2 tyrosine kinase inhibitors.6,9 It is also indicated in the treatment of Ph+ CML in adult patients with the T315I mutation.6
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Treatment of Myeloid leukemia, chronic, chronic phase •••••••••••• ••••• •••••••• ••••••••• •••• •• •••••••• •••••• •••••••••• •••••• Treatment of Myeloid leukemia, chronic, chronic phase •••••••••••• ••••• •••••• - Contraindications & Blackbox Warnings
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Asciminib exerts its therapeutic activity by inhibiting an oncogenic protein responsible for the proliferation of CML. It may be administered orally once or twice a day depending on the condition being treated. By increasing the total daily dose 5-fold as compared to standard therapy (80mg daily vs. 400mg daily), it can be used to treat Ph+ CML with the T315I mutation, a typically treatment-resistant variant of the disease.6
As with many other chemotherapeutic agents, asciminib treatment can result in various forms of myelosuppression, including thrombocytopenia and neutropenia.6 Patients should receive frequent laboratory monitoring throughout therapy and dose adjustments may be required based on the severity of observed effects. Patients may also experience pancreatic and/or cardiovascular toxicity, both of which require frequent monitoring and may require dose adjustments as per prescribing information.6
- Mechanism of action
In most patients with chronic myeloid leukemia (CML),8 progression of the disease is driven primarily by a translocation of the Philadelphia chromosome that creates an oncogenic fusion gene, BCR-ABL1, between the BCR and ABL1 genes.4 This fusion gene produces a resultant fusion protein, BCR-ABL1, which exhibits elevated tyrosine kinase and transforming activities that contribute to CML proliferation.5
Asciminib is an allosteric inhibitor of the BCR-ABL1 tyrosine kinase.6 It binds to the myristoyl pocket of the ABL1 portion of the fusion protein and locks it into an inactive conformation, preventing its oncogenic activity.6,3
Target Actions Organism ATyrosine-protein kinase ABL1 inhibitorallosteric modulatorHumans - Absorption
The median Tmax of asciminib following oral administration is 2.5 hours.6 At a dose of 80mg once daily, the steady-state Cmax and AUCtau were 1781 ng/mL and 15112 ng.h/mL, respectively. At a dose of 40mg twice daily, the steady-state Cmax and AUCtau were 793 ng/mL and 5262 ng.h/mL, respectively. At a dose of 200mg twice daily (for treatment of T315I mutants), the steady-state Cmax and AUCtau were 5642 ng/mL and 37547 ng.h/mL, respectively.6
As compared to the fasted state, the co-administration of asciminib with a high-fat meal decreased the AUC and Cmax by 62% and 68%, respectively, and its co-administration with a low-fat meal decreased the AUC and Cmax by 30% and 35%, respectively.6
- Volume of distribution
At steady-state, the apparent volume of distribution of asciminib is 151 L.6
- Protein binding
In vitro, asciminib is 97% bound to plasma proteins, although the specific protein(s) to which it binds are unclear.6
- Metabolism
Asciminib is negligibly metabolized, with unchanged parent drug comprising the main drug component in plasma (~93%) and following excretion (~57% in feces).6 The main circulating metabolites are M30.5, M44, and M29.5, accounting for approximately 5%, 2%, and 0.4% of the total administered dose, respectively.2 The oxidative metabolism of asciminib is mediated by CYP3A4, and the glucuronidation of asciminib is mediated by UGT2B7 and UGT2B17.6
- Route of elimination
Asciminib is eliminated via biliary secretion facilitated by breast cancer-resistant protein (BCRP) transporters.6 Following oral administration, approximately 80% and 11% of an asciminib dose was recovered in the feces and urine, respectively.6 Unchanged parent drug accounted for 57% of drug material recovered in the feces and 2.5% in the urine.6
- Half-life
The terminal elimination half-life asciminib is 5.5 hours when administered at 40mg twice daily and 9.0 hours when administered at 200mg twice daily.6
- Clearance
The total apparent clearance of asciminib is 6.7 L/h at a total daily dose of 80mg and 4.1 L/h at a dose of 200mg twice daily.6
- Adverse Effects
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There are no data regarding overdosage with asciminib. The effects associated with overdosage are likely to be consistent with the adverse effect profile of asciminib, and may therefore include significant hematological abnormalities and/or gastrointestinal effects, amongst others.6
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- 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 softwareAbacavir The metabolism of Abacavir can be decreased when combined with Asciminib. Abametapir The serum concentration of Asciminib can be increased when it is combined with Abametapir. Abemaciclib The serum concentration of Abemaciclib can be increased when it is combined with Asciminib. Abrocitinib The metabolism of Abrocitinib can be decreased when combined with Asciminib. Acalabrutinib The serum concentration of Acalabrutinib can be increased when it is combined with Asciminib. - Food Interactions
- Take on an empty stomach. Avoid food consumption for at least 2 hours before and 1 hour after taking asciminib.
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.- Product Ingredients
Ingredient UNII CAS InChI Key Asciminib hydrochloride C5U34S9XFV 2119669-71-3 HGCOOPLEWPBLOY-PFEQFJNWSA-N - International/Other Brands
- Scemblix (Novartis AG)
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Scemblix Tablet, film coated 40 mg Oral Novartis Europharm Limited 2022-09-13 Not applicable EU 
Scemblix Tablet 40 mg Oral Novartis 2022-09-01 Not applicable Canada 
Scemblix Tablet, film coated 20 mg/1 Oral Novartis Pharmaceuticals Corporation 2021-10-29 Not applicable US 
Scemblix Tablet, film coated 40 mg Oral Novartis Europharm Limited 2023-02-08 Not applicable EU Scemblix Tablet, film coated 20 mg Oral Novartis Europharm Limited 2022-09-13 Not applicable EU
Categories
- ATC Codes
- L01EA06 — Asciminib
- Drug Categories
- Antineoplastic Agents
- Antineoplastic and Immunomodulating Agents
- Bcr-Abl Tyrosine Kinase Inhibitors
- BCRP/ABCG2 Inhibitors
- BCRP/ABCG2 Substrates
- Cytochrome P-450 CYP2C19 Inhibitors
- Cytochrome P-450 CYP2C19 inhibitors (strength unknown)
- Cytochrome P-450 CYP2C19 Substrates
- Cytochrome P-450 CYP2C9 Inhibitors
- Cytochrome P-450 CYP2C9 Inhibitors (strength unknown)
- Cytochrome P-450 CYP3A Inhibitors
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Inhibitors
- Cytochrome P-450 CYP3A4 Inhibitors (strength unknown)
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 Enzyme Inhibitors
- Cytochrome P-450 Substrates
- Enzyme Inhibitors
- Nicotinic Acids
- OATP1B1/SLCO1B1 Inhibitors
- OATP1B3 inhibitors
- OCT1 inhibitors
- P-glycoprotein inhibitors
- P-glycoprotein substrates
- Protein Kinase Inhibitors
- Pyridines
- Tyrosine Kinase Inhibitors
- UGT1A1 Inhibitors
- UGT2B17 substrates
- UGT2B7 substrates
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as aromatic anilides. These are aromatic compounds containing an anilide group in which the carboxamide group is substituted with an aromatic group. They have the general structure RNC(=O)R', where R= benzene, and R = aryl group.
- Kingdom
- Organic compounds
- Super Class
- Benzenoids
- Class
- Benzene and substituted derivatives
- Sub Class
- Anilides
- Direct Parent
- Aromatic anilides
- Alternative Parents
- Pyrazolylpyridines / Nicotinamides / Dialkylarylamines / Phenol ethers / Phenoxy compounds / Aminopyridines and derivatives / Imidolactams / Heteroaromatic compounds / Pyrrolidines / Pyrazoles show 10 more
- Substituents
- 3-pyrazolylpyridine / Alcohol / Alkyl chloride / Alkyl fluoride / Alkyl halide / Amine / Aminopyridine / Aromatic anilide / Aromatic heteromonocyclic compound / Azacycle show 28 more
- Molecular Framework
- Aromatic heteromonocyclic compounds
- External Descriptors
- Not Available
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- L1F3R18W77
- CAS number
- 1492952-76-7
- InChI Key
- VOVZXURTCKPRDQ-CQSZACIVSA-N
- InChI
- InChI=1S/C20H18ClF2N5O3/c21-20(22,23)31-15-3-1-13(2-4-15)26-19(30)12-9-16(17-5-7-25-27-17)18(24-10-12)28-8-6-14(29)11-28/h1-5,7,9-10,14,29H,6,8,11H2,(H,25,27)(H,26,30)/t14-/m1/s1
- IUPAC Name
- N-[4-(chlorodifluoromethoxy)phenyl]-6-[(3R)-3-hydroxypyrrolidin-1-yl]-5-(1H-pyrazol-5-yl)pyridine-3-carboxamide
- SMILES
- O[C@@H]1CCN(C1)C1=C(C=C(C=N1)C(=O)NC1=CC=C(OC(F)(F)Cl)C=C1)C1=CC=NN1
References
- Synthesis Reference
Schoepfer J, Jahnke W, Berellini G, Buonamici S, Cotesta S, Cowan-Jacob SW, Dodd S, Drueckes P, Fabbro D, Gabriel T, Groell JM, Grotzfeld RM, Hassan AQ, Henry C, Iyer V, Jones D, Lombardo F, Loo A, Manley PW, Pelle X, Rummel G, Salem B, Warmuth M, Wylie AA, Zoller T, Marzinzik AL, Furet P: Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1. J Med Chem. 2018 Sep 27;61(18):8120-8135. doi: 10.1021/acs.jmedchem.8b01040. Epub 2018 Sep 7. [PubMed:30137981]
- General References
- Schoepfer J, Jahnke W, Berellini G, Buonamici S, Cotesta S, Cowan-Jacob SW, Dodd S, Drueckes P, Fabbro D, Gabriel T, Groell JM, Grotzfeld RM, Hassan AQ, Henry C, Iyer V, Jones D, Lombardo F, Loo A, Manley PW, Pelle X, Rummel G, Salem B, Warmuth M, Wylie AA, Zoller T, Marzinzik AL, Furet P: Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1. J Med Chem. 2018 Sep 27;61(18):8120-8135. doi: 10.1021/acs.jmedchem.8b01040. Epub 2018 Sep 7. [Article]
- Tran P, Hanna I, Eggimann FK, Schoepfer J, Ray T, Zhu B, Wang L, Priess P, Tian X, Hourcade-Potelleret F, Einolf HJ: Disposition of asciminib, a potent BCR-ABL1 tyrosine kinase inhibitor, in healthy male subjects. Xenobiotica. 2020 Feb;50(2):150-169. doi: 10.1080/00498254.2019.1594449. Epub 2019 May 6. [Article]
- Hou JZ, Ye JC, Pu JJ, Liu H, Ding W, Zheng H, Liu D: Novel agents and regimens for hematological malignancies: recent updates from 2020 ASH annual meeting. J Hematol Oncol. 2021 Apr 21;14(1):66. doi: 10.1186/s13045-021-01077-3. [Article]
- Jones JK, Thompson EM: Allosteric Inhibition of ABL Kinases: Therapeutic Potential in Cancer. Mol Cancer Ther. 2020 Sep;19(9):1763-1769. doi: 10.1158/1535-7163.MCT-20-0069. Epub 2020 Jun 30. [Article]
- Khatri A, Wang J, Pendergast AM: Multifunctional Abl kinases in health and disease. J Cell Sci. 2016 Jan 1;129(1):9-16. doi: 10.1242/jcs.175521. [Article]
- FDA Approved Drug Products: Scemblix (asciminib) tablets for oral use [Link]
- FDA News Release: FDA approves asciminib for Philadelphia chromosome-positive chronic myeloid leukemia [Link]
- NIH National Cancer Institute: BCR-ABL fusion gene [Link]
- EMA Summary of Product Characteristics: Scemblix (asciminib) film-coated tablets for oral use [Link]
- FDA Approved Drug Products: Scemblix (asciminib) tablets for oral use (June 2023) [Link]
- External Links
- PubChem Compound
- 72165228
- PubChem Substance
- 347828815
- ChemSpider
- 52085218
- BindingDB
- 50459091
- 2584304
- ChEMBL
- CHEMBL4208229
- ZINC
- ZINC000150275965
- PharmGKB
- PA166268841
- PDBe Ligand
- AY7
- Wikipedia
- Asciminib
- PDB Entries
- 5mo4 / 8ssn
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Recruiting Treatment Chronic Myelogenous Leukemia (CML) / Philadelphia Chromosome Positive (Ph+) Chronic Myeloid Leukemia (CML) 1 3 Active Not Recruiting Treatment Chronic Myelogenous Leukemia (CML) 2 3 Active Not Recruiting Treatment Chronic Phase Chronic Myeloid Leukemia 1 3 Active Not Recruiting Treatment Philadelphia Chromosome Positive (Ph+) Chronic Myeloid Leukemia (CML) 1 3 Recruiting Treatment Chronic Myelogenous Leukemia (CML) / Chronic Myeloid Leukemia in Remission / Philadelphia Chromosome Positive (Ph+) Chronic Myeloid Leukemia (CML) 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Tablet, film coated Oral 20 mg Tablet, film coated Oral 40 mg Tablet Oral 20 mg Tablet Oral 40 mg Tablet, film coated Oral 20 mg/1 Tablet, film coated Oral 40 mg/1 - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US8829195 No 2014-09-09 2033-05-13 US US11407735 No 2020-05-14 2040-05-14 US
Properties
- State
- Solid
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source Water Solubility 0.0545 mg/mL ALOGPS logP 3.08 ALOGPS logP 3.4 Chemaxon logS -3.9 ALOGPS pKa (Strongest Acidic) 11.06 Chemaxon pKa (Strongest Basic) 4.19 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 6 Chemaxon Hydrogen Donor Count 3 Chemaxon Polar Surface Area 103.37 Å2 Chemaxon Rotatable Bond Count 6 Chemaxon Refractivity 104.81 m3·mol-1 Chemaxon Polarizability 41.88 Å3 Chemaxon Number of Rings 4 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule Yes Chemaxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS splash10-0a4i-0090000000-5213676570941b43e660 Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-0002-0000900000-4d4b45559b933d704036 Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-0pb9-0080900000-08ba4b18d1d74984a977 Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-06rt-1116900000-f109bbf7bdfb0573af38 Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-000l-0491000000-7dd6c91f0e7a20101617 Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-0059-2793100000-5e2ecad08f23645267a7 Predicted 1H NMR Spectrum 1D NMR Not Applicable Predicted 13C NMR Spectrum 1D NMR Not Applicable - Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 189.88527 predictedDeepCCS 1.0 (2019) [M+H]+ 192.24327 predictedDeepCCS 1.0 (2019) [M+Na]+ 198.33641 predictedDeepCCS 1.0 (2019)
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- InhibitorAllosteric modulator
- General Function
- Syntaxin binding
- Specific Function
- Non-receptor tyrosine-protein kinase that plays a role in many key processes linked to cell growth and survival such as cytoskeleton remodeling in response to extracellular stimuli, cell motility a...
- Gene Name
- ABL1
- Uniprot ID
- P00519
- Uniprot Name
- Tyrosine-protein kinase ABL1
- Molecular Weight
- 122871.435 Da
References
- FDA Approved Drug Products: Scemblix (asciminib) tablets for oral use [Link]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- SubstrateInhibitor
- 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: Scemblix (asciminib) tablets for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Glucuronosyltransferase activity
- Specific Function
- UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds.Its unique specificity for 3,4-catechol estrogens and estriol su...
- Gene Name
- UGT2B7
- Uniprot ID
- P16662
- Uniprot Name
- UDP-glucuronosyltransferase 2B7
- Molecular Weight
- 60694.12 Da
References
- FDA Approved Drug Products: Scemblix (asciminib) tablets for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Glucuronosyltransferase activity
- Specific Function
- UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. The major substrates of this isozyme are eugenol > 4-methylumbe...
- Gene Name
- UGT2B17
- Uniprot ID
- O75795
- Uniprot Name
- UDP-glucuronosyltransferase 2B17
- Molecular Weight
- 61094.915 Da
References
- FDA Approved Drug Products: Scemblix (asciminib) tablets for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- Curator comments
- Asciminib may reversibly inhibit UGT1A1 at plasma concentrations reached at a total daily dose of 80 mg and 200 mg twice daily.
- General Function
- Steroid binding
- Specific Function
- UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform glucuronidates bilirubin IX-alpha to form both the...
- Gene Name
- UGT1A1
- Uniprot ID
- P22309
- Uniprot Name
- UDP-glucuronosyltransferase 1-1
- Molecular Weight
- 59590.91 Da
References
- FDA Approved Drug Products: Scemblix (asciminib) tablets for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- Curator comments
- Asciminib may reversibly inhibit CYP2C19 at concentrations reached at 200 mg twice daily dose.
- General Function
- Steroid hydroxylase activity
- Specific Function
- Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
- Gene Name
- CYP2C19
- Uniprot ID
- P33261
- Uniprot Name
- Cytochrome P450 2C19
- Molecular Weight
- 55930.545 Da
References
- FDA Approved Drug Products: Scemblix (asciminib) tablets for oral use [Link]
- 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
- CYP2C9
- Uniprot ID
- P11712
- Uniprot Name
- Cytochrome P450 2C9
- Molecular Weight
- 55627.365 Da
References
- FDA Approved Drug Products: Scemblix (asciminib) tablets for oral use [Link]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- 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: Scemblix (asciminib) tablets for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- 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: Scemblix (asciminib) tablets for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostagland...
- Gene Name
- SLCO1B1
- Uniprot ID
- Q9Y6L6
- Uniprot Name
- Solute carrier organic anion transporter family member 1B1
- Molecular Weight
- 76447.99 Da
References
- FDA Approved Drug Products: Scemblix (asciminib) tablets for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Mediates the Na(+)-independent uptake of organic anions such as 17-beta-glucuronosyl estradiol, taurocholate, triiodothyronine (T3), leukotriene C4, dehydroepiandrosterone sulfate (DHEAS), methotre...
- Gene Name
- SLCO1B3
- Uniprot ID
- Q9NPD5
- Uniprot Name
- Solute carrier organic anion transporter family member 1B3
- Molecular Weight
- 77402.175 Da
References
- FDA Approved Drug Products: Scemblix (asciminib) tablets for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- General Function
- Secondary active organic cation transmembrane transporter activity
- Specific Function
- Translocates a broad array of organic cations with various structures and molecular weights including the model compounds 1-methyl-4-phenylpyridinium (MPP), tetraethylammonium (TEA), N-1-methylnico...
- Gene Name
- SLC22A1
- Uniprot ID
- O15245
- Uniprot Name
- Solute carrier family 22 member 1
- Molecular Weight
- 61153.345 Da
References
- FDA Approved Drug Products: Scemblix (asciminib) tablets for oral use [Link]
Drug created at October 20, 2016 23:07 / Updated at July 01, 2023 10:08