Identification
- Summary
Ertugliflozin is a SGLT2 inhibitor used to treat type 2 diabetes mellitus.
- Brand Names
- Segluromet, Steglatro, Steglujan
- Generic Name
- Ertugliflozin
- DrugBank Accession Number
- DB11827
- Background
Ertugliflozin belongs to the class of potent and selective inhibitors of the sodium-dependent glucose cotransporters (SGLT), more specifically the type 2 which is responsible for about 90% of the glucose reabsorption from glomerulus.1 This drug was developed under the collaboration of Merck and Pfizer. It was FDA approved as monotherapy and in combination with sitagliptin or metformin hydrochloride on December 22, 2017.6
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
Structure for Ertugliflozin (DB11827)
- Weight
- Average: 436.89
Monoisotopic: 436.1288808 - Chemical Formula
- C22H25ClO7
- Synonyms
- Ertugliflozin
- External IDs
- Pf 04971729
- PF-04971729-00
Pharmacology
- Indication
Ertugliflozin is indicated as an adjunct to diet and exercise to improve glycemic control in adult patients with type 2 diabetes mellitus.10 It is also available in combination with either metformin or sitagliptin for the same indication.7,8
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- Contraindications & Blackbox Warnings
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Administration of ertugliflozin increases urinary glucose excretion which leads to a negative balance and osmotic diuresis. Thus, this antidiabetic agent has been reported to significantly reduce the body weight and blood pressure of diabetic patients.4
- Mechanism of action
As part of a normal process, the glucose from the blood is filtered for excretion and reabsorbed in the glomerulus so less than one percent of this glucose is excreted in the urine. The reabsorption is mediated by the sodium-dependent glucose cotransporter (SGLT), mainly the type 2 which is responsible for 90% of the reabsorbed glucose. Ertugliflozin is a small inhibitor of the SGLT2 and its activity increases glucose excretion, reducing hyperglycemia without the requirement of excessive insulin secretion.1
Target Actions Organism ASodium/glucose cotransporter 2 antagonistHumans - Absorption
Preclinical studies showed that ertugliflozin is well absorbed and had an oral bioavailability of 70-90%. The reported Tmax occurred at 0.5-1.5 hours after dosage.3 Following oral administration, the Cmax and AUC appeared to be dose proportional.Administration of 15 mg reported values of Cmax and AUC of 268 ng/ml and 1193 ng h/ml respectively.9
- Volume of distribution
After oral administration of ertugliflozin, the apparent volume of distribution was reported to be 215.3 L. The steady-state volume of distribution after intravenous administration of etrugliflozin is 85.53 L.9
- Protein binding
Ertugliflozin is highly bound to plasma proteins and it binds in a range of 94-96% independently of the administered concentration.5
- Metabolism
In vitro studies showed that the metabolic profile of ertugliflozin in liver microsomes and hepatocytes is formed by reactions of monohydroxylation, O-demethylation and glucuronidation. The metabolism of ertugliflozin is proposed to be formed by 8 different metabolites found in plasma, feces and urine. In plasma, the unchanged form of ertugliflozin was found to be the major component of the administered dose. There were also other six minor metabolites identified in circulating plasma.3
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- Route of elimination
The total recovery of ertugliflozin was 91% and this elimination route is distributed in a ratio of 50% in the urine and 41% in feces. The recovery of the administered dose was achieved approximately 168 hours after initial administration. Urine elimination occurred very rapidly and 80% of the dosage recovered in urine was obtained after 24 hours. The eliminated dose in urine was composed of seven different major metabolites and the unchanged ertugliflozin as a minor metabolite. The elimination rate in feces was depending on the bowel movements of each patient but 98.5% of the eliminated dose in feces was obtained after 168 hours of initial dosage. This eliminated dose was formed mainly by unchanged ertugliflozin and three other minor metabolites.2
- Half-life
The terminal elimination half-life of ertugliflozin is 11-17 hours.3
- Clearance
The apparent total plasma clearance rate after oral administration of ertugliflozin is 178.7 ml/min and the systemic total plasma clearance after intravenous administration is reported to be 187.2 ml/min.9
- Adverse Effects
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The reports from clinical trials have portrait ertugliflozin to be well tolerated and abscent of significant side effects.5 Carcinogenic studies have been performed and it has been reported an increased incidence of adrenal medullary pheochromocytoma; possibly related to carbohydrate malabsorption leading to altered calcium homeostasis. There were no reported cases of mutagenesis or impairment in fertility.Label
- 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 softwareAbacavir The metabolism of Abacavir can be decreased when combined with Ertugliflozin. Abemaciclib Abemaciclib may decrease the excretion rate of Ertugliflozin which could result in a higher serum level. Abrocitinib The serum concentration of Ertugliflozin can be increased when it is combined with Abrocitinib. Acarbose The therapeutic efficacy of Acarbose can be increased when used in combination with Ertugliflozin. Acebutolol The therapeutic efficacy of Ertugliflozin can be increased when used in combination with Acebutolol. Acetaminophen The metabolism of Acetaminophen can be decreased when combined with Ertugliflozin. Acetazolamide The therapeutic efficacy of Ertugliflozin can be increased when used in combination with Acetazolamide. Acetohexamide The therapeutic efficacy of Acetohexamide can be increased when used in combination with Ertugliflozin. Acetyl sulfisoxazole The therapeutic efficacy of Ertugliflozin can be increased when used in combination with Acetyl sulfisoxazole. Acetylsalicylic acid The risk or severity of hypoglycemia can be increased when Acetylsalicylic acid is combined with Ertugliflozin. 
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- Avoid excessive or chronic alcohol consumption. Alcohol abuse may increase the risk of ketoacidosis.
- 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.- Product Ingredients
Ingredient UNII CAS InChI Key Ertugliflozin pidolate MLU731K321 1210344-83-4 YHIUPZFKHZTLSH-LXYIGGQGSA-N - Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Steglatro Tablet, film coated 5 mg Oral Merck Sharp & Dohme B.V. 2020-12-16 Not applicable EU 
Steglatro Tablet, film coated 15 mg Oral Merck Sharp & Dohme B.V. 2020-12-16 Not applicable EU Steglatro Tablet, film coated 5 mg/1 Oral A-S Medication Solutions 2017-12-19 Not applicable US 
Steglatro Tablet 5 mg Oral Merck Ltd. 2018-05-28 2021-02-03 Canada 
Steglatro Tablet, film coated 15 mg Oral Merck Sharp & Dohme B.V. 2020-12-16 Not applicable EU Steglatro Tablet, film coated 15 mg Oral Merck Sharp & Dohme B.V. 2020-12-16 Not applicable EU Steglatro Tablet, film coated 5 mg Oral Merck Sharp & Dohme B.V. 2020-12-16 Not applicable EU Steglatro Tablet, film coated 5 mg Oral Merck Sharp & Dohme B.V. 2020-12-16 Not applicable EU Steglatro Tablet, film coated 5 mg Oral Merck Sharp & Dohme B.V. 2020-12-16 Not applicable EU Steglatro Tablet, film coated 15 mg/1 Oral A-S Medication Solutions 2017-12-19 Not applicable US - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Segluromet Ertugliflozin (2.5 mg) + Metformin hydrochloride (500 mg) Tablet Oral Merck Ltd. 2018-07-06 2021-02-03 Canada Segluromet Ertugliflozin pidolate (2.5 mg) + Metformin hydrochloride (850 mg) Tablet, film coated Oral Merck Sharp & Dohme B.V. 2020-12-16 Not applicable EU Segluromet Ertugliflozin pidolate (7.5 mg) + Metformin hydrochloride (850 mg) Tablet, film coated Oral Merck Sharp & Dohme B.V. 2020-12-16 Not applicable EU Segluromet Ertugliflozin pidolate (7.5 mg/1) + Metformin hydrochloride (1000 mg/1) Tablet, film coated Oral Merck Sharp & Dohme Llc 2017-12-19 Not applicable US Segluromet Ertugliflozin pidolate (2.5 mg) + Metformin hydrochloride (1000 mg) Tablet, film coated Oral Merck Sharp & Dohme B.V. 2020-12-16 Not applicable EU Segluromet Ertugliflozin pidolate (7.5 mg) + Metformin hydrochloride (1000 mg) Tablet, film coated Oral Merck Sharp & Dohme B.V. 2020-12-16 Not applicable EU Segluromet Ertugliflozin pidolate (2.5 mg/1) + Metformin hydrochloride (500 mg/1) Tablet, film coated Oral Merck Sharp & Dohme Llc 2017-12-19 Not applicable US Segluromet Ertugliflozin pidolate (7.5 mg/1) + Metformin hydrochloride (1000 mg/1) Tablet, film coated Oral A-S Medication Solutions 2017-12-19 Not applicable US Segluromet Ertugliflozin pidolate (2.5 mg) + Metformin hydrochloride (1000 mg) Tablet, film coated Oral Merck Sharp & Dohme B.V. 2020-12-16 Not applicable EU Segluromet Ertugliflozin pidolate (7.5 mg) + Metformin hydrochloride (1000 mg) Tablet, film coated Oral Merck Sharp & Dohme B.V. 2020-12-16 Not applicable EU
Categories
- ATC Codes
- A10BD23 — Metformin and ertugliflozin
- A10BD — Combinations of oral blood glucose lowering drugs
- A10B — BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS
- A10 — DRUGS USED IN DIABETES
- A — ALIMENTARY TRACT AND METABOLISM
- A10BK — Sodium-glucose co-transporter 2 (SGLT2) inhibitors
- A10B — BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS
- A10 — DRUGS USED IN DIABETES
- A — ALIMENTARY TRACT AND METABOLISM
- Drug Categories
- Alimentary Tract and Metabolism
- BCRP/ABCG2 Substrates
- Blood Glucose Lowering Agents
- Diuretics
- Drugs Used in Diabetes
- P-glycoprotein substrates
- Sodium-glucose Cotransporter 2 (SGLT2) Inhibitors
- Sodium-Glucose Transporter 2 Inhibitors
- UGT1A1 Inhibitors
- UGT1A4 Inhibitors
- UGT1A9 Substrates
- UGT2B7 substrates
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as diphenylmethanes. These are compounds containing a diphenylmethane moiety, which consists of a methane wherein two hydrogen atoms are replaced by two phenyl groups.
- Kingdom
- Organic compounds
- Super Class
- Benzenoids
- Class
- Benzene and substituted derivatives
- Sub Class
- Diphenylmethanes
- Direct Parent
- Diphenylmethanes
- Alternative Parents
- Phenoxy compounds / Phenol ethers / Alkyl aryl ethers / Oxepanes / Chlorobenzenes / Ketals / Oxanes / Aryl chlorides / Monosaccharides / 1,3-dioxolanes show 6 more
- Substituents
- Acetal / Alcohol / Alkyl aryl ether / Aromatic heteropolycyclic compound / Aryl chloride / Aryl halide / Chlorobenzene / Diphenylmethane / Ether / Halobenzene show 17 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- Not Available
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 6C282481IP
- CAS number
- 1210344-57-2
- InChI Key
- MCIACXAZCBVDEE-CUUWFGFTSA-N
- InChI
- InChI=1S/C22H25ClO7/c1-2-28-16-6-3-13(4-7-16)9-14-10-15(5-8-17(14)23)22-20(27)18(25)19(26)21(11-24,30-22)12-29-22/h3-8,10,18-20,24-27H,2,9,11-12H2,1H3/t18-,19-,20+,21-,22-/m0/s1
- IUPAC Name
- (1S,2S,3S,4R,5S)-5-{4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl}-1-(hydroxymethyl)-6,8-dioxabicyclo[3.2.1]octane-2,3,4-triol
- SMILES
- CCOC1=CC=C(CC2=CC(=CC=C2Cl)[C@]23OC[C@](CO)(O2)[C@@H](O)[C@H](O)[C@H]3O)C=C1
References
- General References
- Miao Z, Nucci G, Amin N, Sharma R, Mascitti V, Tugnait M, Vaz AD, Callegari E, Kalgutkar AS: Pharmacokinetics, metabolism, and excretion of the antidiabetic agent ertugliflozin (PF-04971729) in healthy male subjects. Drug Metab Dispos. 2013 Feb;41(2):445-56. doi: 10.1124/dmd.112.049551. Epub 2012 Nov 20. [Article]
- Dendup T, Feng X, Clingan S, Astell-Burt T: Environmental Risk Factors for Developing Type 2 Diabetes Mellitus: A Systematic Review. Int J Environ Res Public Health. 2018 Jan 5;15(1). pii: ijerph15010078. doi: 10.3390/ijerph15010078. [Article]
- Abdul-Ghani MA, DeFronzo RA: Inhibition of renal glucose reabsorption: a novel strategy for achieving glucose control in type 2 diabetes mellitus. Endocr Pract. 2008 Sep;14(6):782-90. doi: 10.4158/EP.14.6.782. [Article]
- Kalgutkar AS, Tugnait M, Zhu T, Kimoto E, Miao Z, Mascitti V, Yang X, Tan B, Walsky RL, Chupka J, Feng B, Robinson RP: Preclinical species and human disposition of PF-04971729, a selective inhibitor of the sodium-dependent glucose cotransporter 2 and clinical candidate for the treatment of type 2 diabetes mellitus. Drug Metab Dispos. 2011 Sep;39(9):1609-19. doi: 10.1124/dmd.111.040675. Epub 2011 Jun 20. [Article]
- Cinti F, Moffa S, Impronta F, Cefalo CM, Sun VA, Sorice GP, Mezza T, Giaccari A: Spotlight on ertugliflozin and its potential in the treatment of type 2 diabetes: evidence to date. Drug Des Devel Ther. 2017 Oct 3;11:2905-2919. doi: 10.2147/DDDT.S114932. eCollection 2017. [Article]
- Pfizer News [Link]
- FDA Approved Drug Products: Segluromet (ertugliflozin and metformin hydrochloride) tablets for oral use [Link]
- FDA Approved Drug Products: Steglujan (ertugliflozin and sitagliptin) tablets for oral use [Link]
- Clinical trials [Link]
- FDA Approved Drug Products: Steglatro (ertugliflozin) tablets for oral use [Link]
- External Links
- PubChem Compound
- 44814423
- PubChem Substance
- 347828173
- ChemSpider
- 26340533
- BindingDB
- 50342885
- 1992672
- ChEMBL
- CHEMBL1770248
- ZINC
- ZINC000068197809
- Wikipedia
- Ertugliflozin
- FDA label
- Download (779 KB)
- MSDS
- Download (23.8 KB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Not Yet Recruiting Treatment Fibrosis, Liver / Glycemic Control / Liver Fat / Tolerance / Waist Circumference / Weight Changes 1 4 Not Yet Recruiting Treatment Sleep Apnea 1 4 Recruiting Prevention Diabetic Kidney Disease (DKD) / Diabetic Nephropathy / Ertugliflozin / Kidney Hypoxia / Renoprotection / SGLT2 Inhibitor / Type 2 Diabetes Mellitus 1 4 Recruiting Treatment Congestion / Hearth Failure With Reduced Ejection Fraction (HFrEF) 1 4 Recruiting Treatment Coronavirus Disease 2019 (COVID‑19) 1 4 Recruiting Treatment Heart Failure, Diastolic / Type 2 Diabetes Mellitus 1 4 Withdrawn Treatment Hypertension / Type 2 Diabetes Mellitus 1 4 Withdrawn Treatment Type 2 Diabetes Mellitus 1 3 Active Not Recruiting Treatment Mitral Valve Insufficiency / Systolic Left Ventricular Dysfunction 1 3 Completed Treatment Type 2 Diabetes Mellitus 9
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Tablet Oral Tablet Oral 15 mg Tablet Oral 5 mg Tablet, film coated Oral 15 mg/1 Tablet, film coated Oral 15 MG Tablet, film coated Oral 5 MG Tablet, film coated Oral 5 mg/1 Tablet, film coated Oral Tablet, film coated Oral Tablet, coated Oral Tablet, coated Oral 15 mg Tablet, coated Oral 5 mg - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US7326708 Yes 2008-02-05 2027-05-24 US US6699871 Yes 2004-03-02 2023-01-26 US US6890898 No 2005-05-10 2019-02-02 US US7078381 No 2006-07-18 2019-02-02 US US7459428 No 2008-12-02 2019-02-02 US US8080580 No 2011-12-20 2030-07-13 US US9439902 No 2016-09-13 2030-10-21 US US9439901 No 2016-09-13 2030-10-21 US US9308204 No 2016-04-12 2030-10-21 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source water solubility Very slightly soluble 'FDA label' - Predicted Properties
Property Value Source Water Solubility 0.119 mg/mL ALOGPS logP 2.21 ALOGPS logP 2.32 Chemaxon logS -3.6 ALOGPS pKa (Strongest Acidic) 11.98 Chemaxon pKa (Strongest Basic) -3.1 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 7 Chemaxon Hydrogen Donor Count 4 Chemaxon Polar Surface Area 108.61 Å2 Chemaxon Rotatable Bond Count 6 Chemaxon Refractivity 109.07 m3·mol-1 Chemaxon Polarizability 44.95 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 Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available
Targets
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- 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
- Miao Z, Nucci G, Amin N, Sharma R, Mascitti V, Tugnait M, Vaz AD, Callegari E, Kalgutkar AS: Pharmacokinetics, metabolism, and excretion of the antidiabetic agent ertugliflozin (PF-04971729) in healthy male subjects. Drug Metab Dispos. 2013 Feb;41(2):445-56. doi: 10.1124/dmd.112.049551. Epub 2012 Nov 20. [Article]
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
- Sahasrabudhe V, Terra SG, Hickman A, Saur D, Shi H, O'Gorman M, Zhou Z, Cutler DL: The Effect of Renal Impairment on the Pharmacokinetics and Pharmacodynamics of Ertugliflozin in Subjects With Type 2 Diabetes Mellitus. J Clin Pharmacol. 2017 Nov;57(11):1432-1443. doi: 10.1002/jcph.955. Epub 2017 Jul 13. [Article]
- 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
- Sahasrabudhe V, Terra SG, Hickman A, Saur D, Shi H, O'Gorman M, Zhou Z, Cutler DL: The Effect of Renal Impairment on the Pharmacokinetics and Pharmacodynamics of Ertugliflozin in Subjects With Type 2 Diabetes Mellitus. J Clin Pharmacol. 2017 Nov;57(11):1432-1443. doi: 10.1002/jcph.955. Epub 2017 Jul 13. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- 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
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- General Function
- Protein homodimerization activity
- 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
- UGT1A4
- Uniprot ID
- P22310
- Uniprot Name
- UDP-glucuronosyltransferase 1-4
- Molecular Weight
- 60024.535 Da
Carriers
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- 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
- Cinti F, Moffa S, Impronta F, Cefalo CM, Sun VA, Sorice GP, Mezza T, Giaccari A: Spotlight on ertugliflozin and its potential in the treatment of type 2 diabetes: evidence to date. Drug Des Devel Ther. 2017 Oct 3;11:2905-2919. doi: 10.2147/DDDT.S114932. eCollection 2017. [Article]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- 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
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- 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
Drug created at October 20, 2016 20:51 / Updated at March 24, 2023 20:20