Identification
- Summary
Ivosidenib is an isocitrate dehydrogenase-1 inhibitor used to treat acute myeloid leukemia and cholangiocarcinoma in adults with a susceptible IDH1 mutation.
- Brand Names
- Tibsovo
- Generic Name
- Ivosidenib
- DrugBank Accession Number
- DB14568
- Background
Ivosidenib is a first-in-class isocitrate dehydrogenase-1 (IDH1) inhibitor. IDH1 is an enzyme that is often mutated and overexpressed in some cancers, leading to aberrant cell growth and proliferation.6 Ivosidenib inhibits mutated IDH1, blocking the enzymatic activity and further differentiation of cancer cells.5
Ivosidenib was granted accelerated approval by the FDA in July 2018 for the treatment of relapsed of refractory acute myeloid leukemia in adults.5 It is currently approved to also treat newly diagnosed acute myeloid leukemia in older adults in combination azacitidine or as monotherapy, as well as locally advanced or metastatic cholangiocarcinoma and relapsed or refractory myelodysplastic syndromes in adults. The drug is only effective in patients with a susceptible IDH1 mutation.14
In February 2023, the EMA's Committee for Medicinal Products for Human Use (CHMP) adopted a positive opinion of ivosidenib and recommended it be granted marketing authorization for the treatment of acute myeloid leukemia and cholangiocarcinoma.10 It was fully approved by the EMA in May 2023.13
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
Structure for Ivosidenib (DB14568)
- Weight
- Average: 582.97
Monoisotopic: 582.1394008 - Chemical Formula
- C28H22ClF3N6O3
- Synonyms
- Ivosidenib
- External IDs
- AG-120
Pharmacology
- Indication
Ivosidenib is an isocitrate dehydrogenase-1 (IDH1) inhibitor approved for use in the US and Europe. It is indicated for the treatment of patients with a susceptible IDH1 mutation with:
Newly Diagnosed Acute Myeloid Leukemia (AML) in combination azacitidine or as monotherapy for the treatment of newly diagnosed AML in adults who have comorbidities that preclude the use of intensive induction chemotherapy.9,12 this indication is reserved for adults 75 years or older in the US.9
Relapsed or refractory AML in adults in the US.9
Locally Advanced or Metastatic Cholangiocarcinoma in adults who have been previously treated.9,12
Relapsed or Refractory Myelodysplastic Syndromes in adults.14
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 Used in combination to treat Acute myeloid leukemia (aml) Regimen in combination with: Azacitidine (DB00928) •••••••••••• ••••• •••• •••• ••••••••• ••••• •••••••••• ••• ••••••••• ••• •••••••• ••••••••• ••••••• •••••• Used in combination to treat Acute myeloid leukemia (aml) Regimen in combination with: Azacitidine (DB00928) •••••••••••• ••••• ••••• •••••••••• •••• •••• •••••••• •••••• Treatment of Acute myeloid leukemia (aml) •••••••••••• ••••• ••••• •••••••••• •••• •••• •••••••• •••••• Treatment of Locally advanced cholangiocarcinoma •••••••••••• ••••• •••••••••• •••••••• •••• •••• •••••••• •••••• Treatment of Metastatic cholangiocarcinoma •••••••••••• ••••• •••• •••• ••••••••• •••••••••• ••••••• •••••• - Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- Pharmacodynamics
Ivosidenib is an antineoplastic agent that is effective in cancers with a susceptible IDH1 mutation, which indicates increased levels of oncometabolite D-2-hydroxyglutarate (D-2HG) in cancer cells.5 Ivosidenib decreases D-2HG levels in a dose-dependent manner by inhibiting the IDH1 enzyme. Ivosidenib inhibits both the mutant and wild-type IDH1 but does not inhibit IDH2.7
- Mechanism of action
Isocitrate dehydrogenase 1 (IDH1) is a metabolic enzyme in the cytoplasm and peroxisomes that plays a role in many cellular processes, including mitochondrial oxidative phosphorylation, glutamine metabolism, lipogenesis, glucose sensing, and regulation of cellular redox status.1 IDH1 converts isocitrate to α-ketoglutarate (α-KG), a normal metabolite in the carboxylic acid cycle.1 Multiple cancers are associated with missense mutations in IDH1, leading to the substitution of the amino acid arginine 132 in the enzyme active site, acquired gain-of-function activity, and increased enzyme activity.5,7 IDH1 mutation results in the accumulation of D-2-hydroxyglutarate (D-2HG), an oncometabolite that is structurally similar to α-KG.1,4 D-2HG inhibits α-KG-dependent dioxygenases, including histone and DNA demethylases, which play a role in histone and DNA demethylation along with other cellular processes.4 Inhibition of these enzymes leads to histone and DNA hypermethylation and a block in cell differentiation,1 including hematopoietic differentiation.3 With histone hypermethylation, methylation-sensitive insulators cannot regulate the activation of oncogenes.2 Excess D-2HG ultimately interferes with cellular metabolism and alters epigenetic regulation towards oncogenesis.1,4
Ivosidenib inhibits the mutant IDH1 at much lower concentrations than the wild-type enzyme.9 It targets gene mutations at position R132, with R132H and R132C being the most common mutations.5 In mouse xenograft models of IDH1-mutated AML, ivosidenib caused a decrease in D-2HG levels in a dose-dependent manner and induced myeloid differentiation in vitro and in vivo.9 Ivosidenib works to inhibit histone demethylases and restore normal methylation conditions to promote cell differentiation and oncogene regulation.4
Target Actions Organism AIsocitrate dehydrogenase [NADP] cytoplasmic inhibitorHumans - Absorption
Following oral administration, ivosidenib is rapidly absorbed.7 The Cmax following a single oral dose is 4503 ng/mL in patients with relapsed or refractory AML, 4820 ng/mL in patients with newly diagnosed AML who were also treated with azacitidine, and 4060 ng/mL in patients with cholangiocarcinoma. The steady-state was reached within 14 days. The steady-state Cmax is 6551 ng/mL in patients with relapsed or refractory AML, 6145 ng/mL in patients with newly diagnosed AML who were also treated with azacitidine, and 4799 ng/mL in patients with cholangiocarcinoma. The Tmax ranges from two to three hours.9
A high-fat meal increases ivosidenib exposure.9
- Volume of distribution
The apparent volume of distribution at steady state is 403 L in patients with relapsed or refractory AML, 504 L in patients with newly diagnosed AML who were also treated with azacitidine, and 706 L in patients with cholangiocarcinoma.9
- Protein binding
In vitro, ivosidenib is 92-96% bound to plasma proteins.9
- Metabolism
Ivosidenib is predominantly metabolized by CYP3A4 via oxidation. The exact chemical structures of the metabolites formed from CYP3A4-mediated oxidation have not been fully characterized. Ivosidenib can also undergo N-dealkylation and hydrolysis as minor metabolic pathways.7,8,9
Hover over products below to view reaction partners
- Route of elimination
Following oral administration of ivosidenib, about 77% of the dose was eliminated in feces, where 67% was in the form of unchanged parent drug. About 17% of the dose was excreted in urine, where 10% was in the form of unchanged ivosidenib.9
- Half-life
The terminal half-life at steady state is 58 hours in patients with relapsed or refractory AML, 98 hours in patients with newly diagnosed AML who were also treated with azacitidine, and 129 hours in patients with cholangiocarcinoma.9
- Clearance
The apparent clearance at steady state is 5.6 L/h in patients with relapsed or refractory AML, 4.6 L/h in patients with newly diagnosed AML who were also treated with azacitidine, and 6.1 L/h in patients with cholangiocarcinoma.9
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
There is limited information regarding the LD50 or overdose of ivosidenib.
Ivosidenib is associated with a risk of differentiation syndrome, Guillain-Barre syndrome, and embryo-fetal toxicity.6,9
- 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 software1,2-Benzodiazepine The metabolism of 1,2-Benzodiazepine can be increased when combined with Ivosidenib. Abametapir The serum concentration of Ivosidenib can be increased when it is combined with Abametapir. Abatacept The metabolism of Ivosidenib can be increased when combined with Abatacept. Abemaciclib The metabolism of Abemaciclib can be increased when combined with Ivosidenib. Abiraterone The metabolism of Abiraterone can be increased when combined with Ivosidenib. - Food Interactions
- Do not take with or immediately after a high-fat meal. Administration of ivosidenib with a high-fat meal increases the Cmax and AUC of ivosidenib by 98 and 25%, respectively.
- Exercise caution with grapefruit products. Grapefruit inhibits CYP3A metabolism, which may increase the serum concentration of ivosidenib. Dose adjustment may be necessary if co-administered.
- Exercise caution with St. John's Wort. This herb induces CYP3A metabolism and may reduce serum levels of ivosidenib.
- Take at the same time every day.
- 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 Tibsovo Tablet, film coated 250 mg Oral Les Laboratoires Servier 2023-05-16 Not applicable EU 
Tibsovo Tablet, film coated 250 mg/1 Oral Servier Pharmaceutical LLC 2021-10-19 Not applicable US 
Tibsovo Tablet, film coated 250 mg/1 Oral Agios Pharmaceuticals, Inc. 2018-07-20 2024-11-30 US
Categories
- ATC Codes
- L01XX62 — Ivosidenib
- Drug Categories
- Amino Acids
- Amino Acids, Peptides, and Proteins
- Antineoplastic Agents
- Antineoplastic and Immunomodulating Agents
- Cytochrome P-450 CYP2B6 Inducers
- Cytochrome P-450 CYP2B6 Inducers (strength unknown)
- Cytochrome P-450 CYP2C8 Inducers
- Cytochrome P-450 CYP2C8 Inducers (strength unknown)
- Cytochrome P-450 CYP2C9 Inducers
- Cytochrome P-450 CYP2C9 Inducers (strength unknown)
- Cytochrome P-450 CYP3A Inducers
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Inducers
- Cytochrome P-450 CYP3A4 Inducers (strength unknown)
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 CYP3A4 Substrates with a Narrow Therapeutic Index
- Cytochrome P-450 Enzyme Inducers
- Cytochrome P-450 Substrates
- Enzyme Inhibitors
- Isocitrate Dehydrogenase 1 Inhibitor
- Isocitrate dehydrogenase-1 (IDH1) inhibitors
- Isocitrate Dehydrogenase-1 Inhibitors
- Moderate Risk QTc-Prolonging Agents
- Narrow Therapeutic Index Drugs
- OAT3/SLC22A8 Inhibitors
- P-glycoprotein inhibitors
- P-glycoprotein substrates
- P-glycoprotein substrates with a Narrow Therapeutic Index
- QTc Prolonging Agents
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as proline and derivatives. These are compounds containing proline or a derivative thereof resulting from reaction of proline at the amino group or the carboxy group, or from the replacement of any hydrogen of glycine by a heteroatom.
- Kingdom
- Organic compounds
- Super Class
- Organic acids and derivatives
- Class
- Carboxylic acids and derivatives
- Sub Class
- Amino acids, peptides, and analogues
- Direct Parent
- Proline and derivatives
- Alternative Parents
- Alpha amino acid amides / Phenylacetamides / Pyrrolidinecarboxamides / Chlorobenzenes / Pyrrolidine-2-ones / Pyridines and derivatives / Aryl chlorides / Aryl fluorides / Imidolactams / Tertiary carboxylic acid amides show 11 more
- Substituents
- 2-pyrrolidone / Alkyl fluoride / Alkyl halide / Alpha-amino acid amide / Aromatic heteromonocyclic compound / Aryl chloride / Aryl fluoride / Aryl halide / Azacycle / Benzenoid show 30 more
- Molecular Framework
- Aromatic heteromonocyclic compounds
- External Descriptors
- Not Available
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- Q2PCN8MAM6
- CAS number
- 1448347-49-6
- InChI Key
- WIJZXSAJMHAVGX-DHLKQENFSA-N
- InChI
- InChI=1S/C28H22ClF3N6O3/c29-21-4-2-1-3-20(21)25(26(40)36-18-11-28(31,32)12-18)37(19-10-17(30)14-34-15-19)27(41)22-5-6-24(39)38(22)23-9-16(13-33)7-8-35-23/h1-4,7-10,14-15,18,22,25H,5-6,11-12H2,(H,36,40)/t22-,25-/m0/s1
- IUPAC Name
- (2S)-2-(2-chlorophenyl)-2-{1-[(2S)-1-(4-cyanopyridin-2-yl)-5-oxopyrrolidin-2-yl]-N-(5-fluoropyridin-3-yl)formamido}-N-(3,3-difluorocyclobutyl)acetamide
- SMILES
- [H][C@@](N(C(=O)[C@]1([H])CCC(=O)N1C1=NC=CC(=C1)C#N)C1=CC(F)=CN=C1)(C(=O)NC1CC(F)(F)C1)C1=C(Cl)C=CC=C1
References
- General References
- Mondesir J, Willekens C, Touat M, de Botton S: IDH1 and IDH2 mutations as novel therapeutic targets: current perspectives. J Blood Med. 2016 Sep 2;7:171-80. doi: 10.2147/JBM.S70716. eCollection 2016. [Article]
- Flavahan WA, Drier Y, Liau BB, Gillespie SM, Venteicher AS, Stemmer-Rachamimov AO, Suva ML, Bernstein BE: Insulator dysfunction and oncogene activation in IDH mutant gliomas. Nature. 2016 Jan 7;529(7584):110-4. doi: 10.1038/nature16490. Epub 2015 Dec 23. [Article]
- Figueroa ME, Abdel-Wahab O, Lu C, Ward PS, Patel J, Shih A, Li Y, Bhagwat N, Vasanthakumar A, Fernandez HF, Tallman MS, Sun Z, Wolniak K, Peeters JK, Liu W, Choe SE, Fantin VR, Paietta E, Lowenberg B, Licht JD, Godley LA, Delwel R, Valk PJ, Thompson CB, Levine RL, Melnick A: Leukemic IDH1 and IDH2 mutations result in a hypermethylation phenotype, disrupt TET2 function, and impair hematopoietic differentiation. Cancer Cell. 2010 Dec 14;18(6):553-67. doi: 10.1016/j.ccr.2010.11.015. Epub 2010 Dec 9. [Article]
- Popovici-Muller J, Lemieux RM, Artin E, Saunders JO, Salituro FG, Travins J, Cianchetta G, Cai Z, Zhou D, Cui D, Chen P, Straley K, Tobin E, Wang F, David MD, Penard-Lacronique V, Quivoron C, Saada V, de Botton S, Gross S, Dang L, Yang H, Utley L, Chen Y, Kim H, Jin S, Gu Z, Yao G, Luo Z, Lv X, Fang C, Yan L, Olaharski A, Silverman L, Biller S, Su SM, Yen K: Discovery of AG-120 (Ivosidenib): A First-in-Class Mutant IDH1 Inhibitor for the Treatment of IDH1 Mutant Cancers. ACS Med Chem Lett. 2018 Jan 19;9(4):300-305. doi: 10.1021/acsmedchemlett.7b00421. eCollection 2018 Apr 12. [Article]
- Merchant SL, Culos K, Wyatt H: Ivosidenib: IDH1 Inhibitor for the Treatment of Acute Myeloid Leukemia. J Adv Pract Oncol. 2019 Jul;10(5):494-500. doi: 10.6004/jadpro.2019.10.5.7. Epub 2019 Jul 1. [Article]
- Authors unspecified: Ivosidenib . [Article]
- Dhillon S: Ivosidenib: First Global Approval. Drugs. 2018 Sep;78(14):1509-1516. doi: 10.1007/s40265-018-0978-3. [Article]
- Prakash C, Fan B, Altaf S, Agresta S, Liu H, Yang H: Pharmacokinetics, absorption, metabolism, and excretion of [(14)C]ivosidenib (AG-120) in healthy male subjects. Cancer Chemother Pharmacol. 2019 May;83(5):837-848. doi: 10.1007/s00280-019-03793-7. Epub 2019 Feb 13. [Article]
- FDA Approved Drug Products: TIBSOVO (ivosidenib) tablets, for oral use [Link]
- CHMP Summary of Positive Opinion: Tibsovo (ivosidenib) [Link]
- CHMP Summary of Positive Opinion: Tidhesco (ivosidenib) [Link]
- EMA Approved Drug Products: Tibsovo (ivosidenib) Oral Tablets [Link]
- PR Newswire: Servier receives European Commission approval of Tibsovo® (ivosidenib tablets) in IDH1-mutated Acute Myeloid Leukemia and IDH1-mutated Cholangiocarcinoma [Link]
- FDA Approved Drug Products: TIBSOVO® (ivosidenib tablets), for oral use (October 2023) [Link]
- External Links
- ChemSpider
- 38772333
- BindingDB
- 363689
- 2049873
- ChEBI
- 145430
- ChEMBL
- CHEMBL3989958
- ZINC
- ZINC000205136523
- Wikipedia
- Ivosidenib
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 3 Active Not Recruiting Treatment Acute Myeloid Leukemia / Acute Myeloid Leukemia Arising From Previous Myelodysplastic Syndrome / Newly Diagnosed Acute Myeloid Leukemia (AML) / Treatment Naive AML 1 3 Completed Treatment Cholangiocarcinoma Advanced / Metastatic Cholangiocarcinoma 1 3 Not Yet Recruiting Treatment Biliary Tract Neoplasms 1 3 Not Yet Recruiting Treatment Locally Advanced or Metastatic Conventional Chondrosarcoma With an IDH1 Mutation, Untreated or Previously Treated With 1 Systemic Treatment Regimen 1 3 Recruiting Treatment Acute Myeloid Leukemia 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Tablet, film coated Oral 250 mg Tablet, film coated Oral 250 mg/1 - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US9474779 No 2016-10-25 2033-08-19 US US9850277 No 2017-12-26 2033-01-18 US US9968595 No 2018-05-15 2035-03-13 US US10449184 No 2019-10-22 2035-03-13 US US10610125 No 2020-04-07 2030-06-21 US US10799490 No 2020-10-13 2035-03-13 US US10980788 No 2021-04-20 2039-06-07 US US10717764 No 2020-07-21 2033-01-18 US US10653710 No 2020-05-19 2036-10-18 US US11667673 No 2013-01-18 2033-01-18 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source water solubility <1 mg/mL https://www.selleck.cn/msds/MSDS_S8206.pdf - Predicted Properties
Property Value Source Water Solubility 0.0208 mg/mL ALOGPS logP 2.52 ALOGPS logP 3.01 Chemaxon logS -4.4 ALOGPS pKa (Strongest Acidic) 12.14 Chemaxon pKa (Strongest Basic) 1.81 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 6 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 119.29 Å2 Chemaxon Rotatable Bond Count 7 Chemaxon Refractivity 139.33 m3·mol-1 Chemaxon Polarizability 53.42 Å3 Chemaxon Number of Rings 5 Chemaxon Bioavailability 1 Chemaxon Rule of Five No Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule Yes Chemaxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Not Available
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- Curator comments
- Ivosidenib inhibits both the wild-type and mutant forms of IDH1 with varying affinities.
- General Function
- Receptor binding
- Specific Function
- Not Available
- Gene Name
- IDH1
- Uniprot ID
- O75874
- Uniprot Name
- Isocitrate dehydrogenase [NADP] cytoplasmic
- Molecular Weight
- 46659.005 Da
References
- Megias-Vericat JE, Ballesta-Lopez O, Barragan E, Montesinos P: IDH1-mutated relapsed or refractory AML: current challenges and future prospects. Blood Lymphat Cancer. 2019 Jun 27;9:19-32. doi: 10.2147/BLCTT.S177913. eCollection 2019. [Article]
- Merchant SL, Culos K, Wyatt H: Ivosidenib: IDH1 Inhibitor for the Treatment of Acute Myeloid Leukemia. J Adv Pract Oncol. 2019 Jul;10(5):494-500. doi: 10.6004/jadpro.2019.10.5.7. Epub 2019 Jul 1. [Article]
- FDA Approved Drug Products: TIBSOVO (ivosidenib) tablets, for oral use [Link]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInducer
- 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
- Prakash C, Fan B, Altaf S, Agresta S, Liu H, Yang H: Pharmacokinetics, absorption, metabolism, and excretion of [(14)C]ivosidenib (AG-120) in healthy male subjects. Cancer Chemother Pharmacol. 2019 May;83(5):837-848. doi: 10.1007/s00280-019-03793-7. Epub 2019 Feb 13. [Article]
- FDA Approved Drug Products: TIBSOVO (ivosidenib) tablets, for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inducer
- 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
- CYP2B6
- Uniprot ID
- P20813
- Uniprot Name
- Cytochrome P450 2B6
- Molecular Weight
- 56277.81 Da
References
- FDA Approved Drug Products: TIBSOVO (ivosidenib) tablets, for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inducer
- Curator comments
- There are limited data in the literature supporting this enzyme action, however the FDA label states that ivosidenib may induce CYP2C9.
- 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: TIBSOVO (ivosidenib) tablets, for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inducer
- 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: TIBSOVO (ivosidenib) 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: TIBSOVO (ivosidenib) 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
- Plays an important role in the excretion/detoxification of endogenous and exogenous organic anions, especially from the brain and kidney. Involved in the transport basolateral of steviol, fexofenad...
- Gene Name
- SLC22A8
- Uniprot ID
- Q8TCC7
- Uniprot Name
- Solute carrier family 22 member 8
- Molecular Weight
- 59855.585 Da
References
- FDA Approved Drug Products: TIBSOVO (ivosidenib) tablets, for oral use [Link]
Drug created at July 20, 2018 16:42 / Updated at November 24, 2023 04:34