Identification
- Summary
Sotagliflozin is an orally administered dual SGLT1/2 inhibitor used alongside insulin to improve glycemic control in patients with type 1 diabetes mellitus.
- Brand Names
- Inpefa
- Generic Name
- Sotagliflozin
- DrugBank Accession Number
- DB12713
- Background
Sotagliflozin is a dual inhibitor of SGLT1 and SGLT2, the first of its kind,2 which is approved for use in the EU, in combination with insulin, to improve glycemic control in patients with type 1 diabetes mellitus (T1DM) and a BMI ≥27 kg/m2.3 Its potency in inhibiting SGLT2 is similar to that of other SGLT2 inhibitors, such as canagliflozin and dapagliflozin, but its potency in inhibiting SGLT1 is >10-fold higher than its predecessors.2 The added inhibition of intestinal SGLT1 delays glucose absorption in the distal small intestine and colon, thereby reducing post-prandial glucose levels.1,2
Sotagliflozin was approved by the EMA under the brand name "Zynquista" on April 26, 2019, for the treatment of type 1 diabetes.5 A similar approval has also been sought in the US, but the FDA has since published a proposal to refuse the approval because the data submitted did not show that it was safe under the proposed conditions of use.6 On March 22, 2022, the marketing authorization of sotagliflozin for the treatment of type 1 diabetes mellitus was withdrawn by the EMA due to commercial reasons.8
In May 2023, sotagliflozin was approved by the FDA to reduce the risk of cardiovascular death and heart failure in patients with high risk factors.[]
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
Structure for Sotagliflozin (DB12713)
- Weight
- Average: 424.94
Monoisotopic: 424.1111228 - Chemical Formula
- C21H25ClO5S
- Synonyms
- Sotagliflozin
- External IDs
- LP-802034
- LX4211
Pharmacology
- Indication
In the US, sotagliflozin is indicated to reduce the risk of cardiovascular death and heart failure in adults with heart failure, type 2 diabetes mellitus, chronic kidney disease, and other cardiovascular risk factors.7
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 Prevention of Cardiovascular mortality •••••••••••• ••••• •••••••••••••• •••• Prevention of Cardiovascular mortality •••••••••••• ••••• Prevention of Cardiovascular mortality •••••••••••• ••••• Prevention of Cardiovascular mortality •••••••••••• ••••• Prevention of Heart failure •••••••••••• ••••• ••••• ••••••• •• ••••• ••••••• - 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
Sotagliflozin exerts its pharmacologic effects by slowing glucose absorption in the gastrointestinal tract and increasing the excretion of glucose in the urine.3 It is administered by mouth once daily before the first meal of the day.
The use of SGLT2 inhibitors, including sotagliflozin, can cause diabetic ketoacidosis (DKA). Patients, especially those with a higher baseline risk of DKA, should be instructed on how and when to monitor for ketoacidosis and what actions to take when DKA is suspected.3
SGLT2 inhibitors, including sotagliflozin, also increase the risk of genital infections. This is due to the increase in urinary glucose excretion, which provides a relatively glucose-rich environment in which infectious agents may establish themselves.3
- Mechanism of action
Sodium-glucose co-transporter types 1 and 2 (SGLT1 and SGLT2) are integral in the transport of glucose in the body. SGLT1 is the major transporter for glucose absorption in the gastrointestinal tract,1 while SGLT2 is the predominant transporter responsible for reabsorption of glucose in the glomerulus.3
Sotagliflozin is a dual inhibitor of both SGLT1 and SGLT2.3 Inhibition of SGLT1 results in a delay in glucose absorption and a blunting of postprandial hyperglycemia, while inhibition of SGLT2 reduces renal reabsorption of filtered glucose, thereby increasing urinary glucose excretion.
Target Actions Organism ASodium/glucose cotransporter 2 inhibitorHumans ASodium/glucose cotransporter 1 inhibitorHumans - Absorption
Following a single dose, the Tmax of sotagliflozin ranged from 1.25 to 3 hours.3 Following multiple doses, the Tmax ranged from 2.5 to 4 hours.3 The estimated oral bioavailability of sotagliflozin is 71%.3
- Volume of distribution
Sotagliflozin has a mean apparent volume of distribution of 9392 L.3
- Protein binding
Both sotagliflozin and its major metabolite, M19, are extensively (~98%) protein-bound in plasma, although the specific protein(s) to which they bind have not been elucidated.3
- Metabolism
The major metabolite of sotagliflozin is a 3-O-glucuronide (M19), which comprised ~94% of of the radioactivity in plasma following the oral administration of a radiolabeled dose of sotagliflozin.3 The M19 metabolite is effectively inactive, with >275-fold less activity at SGLT1 and SGLT2 compared to the parent drug.4
The primary route of metabolism is via glucuronidation by UGT1A9 (and both UGT1A1 and UGT2B7, to a lesser extent) as well as oxidation via CYP3A4.3
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- Route of elimination
Sotagliflozin is primarily eliminated via the renal route, with 57% of administered drug material appearing in the urine and 37% appearing in the feces.3
- Half-life
The mean terminal half-life of sotagliflozin ranged from 21 to 35 hours and from 19 to 26 hours for its M19 metabolite.3
- Clearance
In healthy volunteers, the mean apparent clearance of sotagliflozin ranged from 261 to 374 L/h.3 The mean apparent clearance estimated in a population of mostly type 1 diabetic patients was 239 L/h.3
- 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
Multiple doses of 800mg once daily (double the maximum recommended dose) have been administered to healthy volunteers without evidence of overdose symptoms.3 In the event of a suspected overdose, administer supportive treatment as clinically indicated.
- 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 softwareAbemaciclib The serum concentration of Abemaciclib can be increased when it is combined with Sotagliflozin. Acarbose The risk or severity of hypoglycemia can be increased when Acarbose is combined with Sotagliflozin. Acebutolol The therapeutic efficacy of Sotagliflozin can be increased when used in combination with Acebutolol. Acetazolamide The therapeutic efficacy of Sotagliflozin can be increased when used in combination with Acetazolamide. Acetohexamide The risk or severity of hypoglycemia can be increased when Acetohexamide is combined with Sotagliflozin. - Food Interactions
- Take before a meal. Sotagliflozin should be taken once daily before the first meal of the day.
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 Inpefa Tablet 400 mg/1 Oral Lexicon Pharmaceuticals, Inc. 2023-05-26 Not applicable US 
Inpefa Tablet 200 mg/1 Oral Lexicon Pharmaceuticals, Inc. 2023-05-26 Not applicable US Inpefa Tablet 200 mg/1 Oral Lexicon Pharmaceuticals, Inc. 2023-05-26 Not applicable US Inpefa Tablet 400 mg/1 Oral Lexicon Pharmaceuticals, Inc. 2023-05-26 2023-05-26 US Zynquista Tablet, film coated 200 mg Oral Guidehouse Germany Gmb H 2020-12-16 2022-08-16 EU 
Categories
- ATC Codes
- A10BK06 — Sotagliflozin
- Drug Categories
- Alimentary Tract and Metabolism
- BCRP/ABCG2 Inhibitors
- Blood Glucose Lowering Agents
- Cytochrome P-450 CYP2D6 Inhibitors
- Cytochrome P-450 CYP2D6 Inhibitors (strength unknown)
- Cytochrome P-450 CYP3A Inducers
- Cytochrome P-450 CYP3A Inhibitors
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Inducers
- Cytochrome P-450 CYP3A4 Inducers (strength unknown)
- Cytochrome P-450 CYP3A4 Inhibitors
- Cytochrome P-450 CYP3A4 Inhibitors (strength unknown)
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 Enzyme Inducers
- Cytochrome P-450 Enzyme Inhibitors
- Cytochrome P-450 Substrates
- Diuretics
- Drugs Used in Diabetes
- OATP1B1/SLCO1B1 Inhibitors
- OATP1B3 inhibitors
- P-glycoprotein inhibitors
- Sodium-glucose Cotransporter 2 (SGLT2) Inhibitors
- Sodium-Glucose Transporter 1, antagonists & inhibitors
- Sodium-Glucose Transporter 2 Inhibitors
- UGT1A1 Substrates
- UGT1A9 Substrates
- UGT2B7 substrates
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as phenolic glycosides. These are organic compounds containing a phenolic structure attached to a glycosyl moiety. Some examples of phenolic structures include lignans, and flavonoids. Among the sugar units found in natural glycosides are D-glucose, L-Fructose, and L rhamnose.
- Kingdom
- Organic compounds
- Super Class
- Organic oxygen compounds
- Class
- Organooxygen compounds
- Sub Class
- Carbohydrates and carbohydrate conjugates
- Direct Parent
- Phenolic glycosides
- Alternative Parents
- Diphenylmethanes / Thioglycosides / Phenoxy compounds / Phenol ethers / Alkyl aryl ethers / Chlorobenzenes / Aryl chlorides / Oxanes / Monosaccharides / Monothioacetals show 6 more
- Substituents
- Alcohol / Alkyl aryl ether / Aromatic heteromonocyclic compound / Aryl chloride / Aryl halide / Benzenoid / Chlorobenzene / Diphenylmethane / Ether / Halobenzene show 17 more
- Molecular Framework
- Aromatic heteromonocyclic compounds
- External Descriptors
- Not Available
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 6B4ZBS263Y
- CAS number
- 1018899-04-1
- InChI Key
- QKDRXGFQVGOQKS-CRSSMBPESA-N
- InChI
- InChI=1S/C21H25ClO5S/c1-3-26-15-7-4-12(5-8-15)10-14-11-13(6-9-16(14)22)20-18(24)17(23)19(25)21(27-20)28-2/h4-9,11,17-21,23-25H,3,10H2,1-2H3/t17-,18-,19+,20+,21-/m1/s1
- IUPAC Name
- (2S,3R,4R,5S,6R)-2-{4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl}-6-(methylsulfanyl)oxane-3,4,5-triol
- SMILES
- CCOC1=CC=C(CC2=CC(=CC=C2Cl)[C@@H]2O[C@H](SC)[C@@H](O)[C@H](O)[C@H]2O)C=C1
References
- Synthesis Reference
Zhao MM, Zhang H, Iimura S, Bednarz MS, Song Q, Lim N, Yan J, Wu W, Dai K, Gu X, Wang Y: Process Development of Sotagliflozin, a Dual Inhibitor of Sodium–Glucose Cotransporter-1/2 for the Treatment of Diabetes Org Process Res Dev. 2020 Oct 7;24(11):2689-2701.
- General References
- Lapuerta P, Zambrowicz B, Strumph P, Sands A: Development of sotagliflozin, a dual sodium-dependent glucose transporter 1/2 inhibitor. Diab Vasc Dis Res. 2015 Mar;12(2):101-10. doi: 10.1177/1479164114563304. [Article]
- Cefalo CMA, Cinti F, Moffa S, Impronta F, Sorice GP, Mezza T, Pontecorvi A, Giaccari A: Sotagliflozin, the first dual SGLT inhibitor: current outlook and perspectives. Cardiovasc Diabetol. 2019 Feb 28;18(1):20. doi: 10.1186/s12933-019-0828-y. [Article]
- EMA Summary of Product Characteristics: Zynquista (sotagliflozin) film-coated tablets for oral use [Link]
- FDA Endocrinologic And Metabolic Drugs Advisory Committee: Sotagliflozin for the Treatment of Type 1 Diabetes [Link]
- EMA European Public Assessment Report: Zynquista (sotagliflozin) [Link]
- US Federal Register: Proposal To Refuse To Approve a New Drug Application for Sotagliflozin Oral Tablets, 200 Milligrams and 400 Milligrams; Opportunity for a Hearing [Link]
- FDA Approved Drug Products: INPEFA (sotagliflozin) tablets, for oral use (May 2023) [Link]
- EMA Public Statement: Zynquista Withdrawal of the marketing authorisation in the European Union [Link]
- External Links
- PubChem Compound
- 24831714
- PubChem Substance
- 347828911
- ChemSpider
- 27289071
- BindingDB
- 50235017
- 2638675
- ChEMBL
- CHEMBL3039507
- ZINC
- ZINC000095641922
- PDBe Ligand
- LFL
- Wikipedia
- Sotagliflozin
- PDB Entries
- 8hg7
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 Not Yet Recruiting Treatment Albuminuria / Diabetic complications cardiovascular / Diabetic complications renal / Diabetic Nephropathy / Hypoxia / Renal Dysfunction / Type 1 Diabetes Mellitus 1 4 Recruiting Treatment Heart Failure With Preserved Ejection Fraction (HFpEF) 1 3 Completed Treatment Chronic Kidney Disease, Stage 3 (Moderate) / Type 2 Diabetes Mellitus 1 3 Completed Treatment Hyperglycemia / Type 1 Diabetes Mellitus 1 3 Completed Treatment Stage 4 Chronic Kidney Disease / Type 2 Diabetes Mellitus 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Tablet Oral 200 mg/1 Tablet Oral 400 mg/1 Tablet, film coated Oral 200 mg - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US8217156 No 2012-07-10 2030-10-07 US US7781577 No 2010-08-24 2028-05-04 US US8476413 No 2013-07-02 2028-05-29 US
Properties
- State
- Solid
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source Water Solubility 0.042 mg/mL ALOGPS logP 3.19 ALOGPS logP 3.73 Chemaxon logS -4 ALOGPS pKa (Strongest Acidic) 12.47 Chemaxon pKa (Strongest Basic) -3.7 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 5 Chemaxon Hydrogen Donor Count 3 Chemaxon Polar Surface Area 79.15 Å2 Chemaxon Rotatable Bond Count 6 Chemaxon Refractivity 110.87 m3·mol-1 Chemaxon Polarizability 44.93 Å3 Chemaxon Number of Rings 3 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 splash10-004i-0002900000-478a8abbe85c7e279adc Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-00di-2009800000-fa3d65869c3912c814a4 Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-0550-0494300000-d2ae6ac8e3f4af89d4a1 Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-001i-9106100000-ebcf0315522502b4d98a Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-003r-6359100000-b580a97549b7e6684215 Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-0bvl-9178200000-e6ba460ca55ce0a500cc 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]- 188.4029 predictedDeepCCS 1.0 (2019) [M+H]+ 190.79846 predictedDeepCCS 1.0 (2019) [M+Na]+ 197.3679 predictedDeepCCS 1.0 (2019)
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Low-affinity glucose:sodium symporter activity
- Specific Function
- Sodium-dependent glucose transporter. Has a Na(+) to glucose coupling ratio of 1:1.Efficient substrate transport in mammalian kidney is provided by the concerted action of a low affinity high capac...
- Gene Name
- SLC5A2
- Uniprot ID
- P31639
- Uniprot Name
- Sodium/glucose cotransporter 2
- Molecular Weight
- 72895.995 Da
References
- EMA Summary of Product Characteristics: Zynquista (sotagliflozin) film-coated tablets for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Glucose:sodium symporter activity
- Specific Function
- Actively transports glucose into cells by Na(+) cotransport with a Na(+) to glucose coupling ratio of 2:1. Efficient substrate transport in mammalian kidney is provided by the concerted action of a...
- Gene Name
- SLC5A1
- Uniprot ID
- P13866
- Uniprot Name
- Sodium/glucose cotransporter 1
- Molecular Weight
- 73497.275 Da
References
- EMA Summary of Product Characteristics: Zynquista (sotagliflozin) film-coated tablets for oral use [Link]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Retinoic acid binding
- Specific Function
- UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform has specificity for phenols. Isoform 2 lacks trans...
- Gene Name
- UGT1A9
- Uniprot ID
- O60656
- Uniprot Name
- UDP-glucuronosyltransferase 1-9
- Molecular Weight
- 59940.495 Da
References
- EMA Summary of Product Characteristics: Zynquista (sotagliflozin) film-coated tablets for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- 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
- EMA Summary of Product Characteristics: Zynquista (sotagliflozin) film-coated 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
- EMA Summary of Product Characteristics: Zynquista (sotagliflozin) film-coated tablets for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- SubstrateInhibitorInducer
- Curator comments
- M19 (the main metabolite of sotagliflozin) is both an inducer and inhibitor of CYP3A4.
- 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
- EMA Summary of Product Characteristics: Zynquista (sotagliflozin) film-coated tablets for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- Curator comments
- M19 (the main metabolite of sotagliflozin) is an inhibitor of CYP2D6.
- 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
- EMA Summary of Product Characteristics: Zynquista (sotagliflozin) film-coated tablets for oral use [Link]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- Curator comments
- Demonstrated in vitro.
- 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
- EMA Summary of Product Characteristics: Zynquista (sotagliflozin) film-coated tablets for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- Curator comments
- Demonstrated in vitro.
- 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
- EMA Summary of Product Characteristics: Zynquista (sotagliflozin) film-coated tablets for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- Curator comments
- M19 (the main metabolite of sotagliflozin) has demonstrated inhibitory effects against OATP1B1 in vitro.
- 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
- EMA Summary of Product Characteristics: Zynquista (sotagliflozin) film-coated tablets for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- Curator comments
- M19 (the main metabolite of sotagliflozin) has demonstrated inhibitory effects against OATP1B3 in vitro.
- 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
- EMA Summary of Product Characteristics: Zynquista (sotagliflozin) film-coated tablets for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- Curator comments
- M19 (the main metabolite of sotagliflozin) has demonstrated inhibitory effects against MRP2 in vitro.
- General Function
- Organic anion transmembrane transporter activity
- Specific Function
- Mediates hepatobiliary excretion of numerous organic anions. May function as a cellular cisplatin transporter.
- Gene Name
- ABCC2
- Uniprot ID
- Q92887
- Uniprot Name
- Canalicular multispecific organic anion transporter 1
- Molecular Weight
- 174205.64 Da
References
- EMA Summary of Product Characteristics: Zynquista (sotagliflozin) film-coated tablets for oral use [Link]
Drug created at October 20, 2016 23:45 / Updated at May 31, 2023 07:30