Identification
- Summary
Mitapivat is a pyruvate kinase activator used to treat hemolytic anemia in adults with pyruvate kinase (PK) deficiency.
- Brand Names
- Pyrukynd 5 Mg 4-week
- Generic Name
- Mitapivat
- DrugBank Accession Number
- DB16236
- Background
Mitapivat is a novel, first-in-class pyruvate kinase activator. It works to increase the activity of erythrocyte pyruvate kinase, a key enzyme involved in the survival of red blood cells. Defects in the pyruvate kinase enzyme in various red blood cells disorders lead to the lack of energy production for red blood cells, leading to lifelong premature destruction of red blood cells or chronic hemolytic anemia.1
On February 17, 2022, the FDA approved mitapivat as the first disease-modifying treatment for hemolytic anemia in adults with pyruvate kinase (PK) deficiency, a rare, inherited disorder leading to lifelong hemolytic anemia.6 Mitapivat has also been investigated in other hereditary red blood cell disorders associated with hemolytic anemia, such as sickle cell disease and alpha- and beta-thalassemia.1
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
Structure for Mitapivat (DB16236)
- Weight
- Average: 450.56
Monoisotopic: 450.172561887 - Chemical Formula
- C24H26N4O3S
- Synonyms
- Mitapivat
- Pkr-in-1
- External IDs
- AG-348
Pharmacology
- Indication
Mitapivat is indicated for the treatment of hemolytic anemia in adults with pyruvate kinase (PK) deficiency.5
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Treatment of Pyruvate kinase deficiency anaemia •••••••••••• ••••• •••••• - Contraindications & Blackbox Warnings
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Mitapivat is a pyruvate kinase activator that works to increase the activity of erythrocyte pyruvate kinase, an enzyme responsible for energy production for and survival of red blood cells. It is effective in upregulating the activity of both wild-type and mutant forms of erythrocyte pyruvate kinase.1,5
Interestingly, mitapivat is a mild-to-moderate inhibitor of the aromatase enzyme (CYP19A1),1 which is an enzyme involved in biosynthesis of estrogens from androgen precursors. Inhibition of aromatase is associated with bone density loss, as estrogen mediates suppressive, antiresorptive effects on osteoclasts and generally favours bone formation over resorption. Thus, low estrogen levels can increase bone turnover and osteoclast activity, resulting in net bone loss and decreased bone quality.2 Inhibition of aromatase by mitapivat may have some clinical implications, as patients with pyruvate kinase deficiency have considerably high rate of osteopenia and osteoporosis. The long-term effect of mitapivant on bond mineral density requires further investigation. One study suggests that this off-target effect may have negligible clinical effects on adults, but may potentially have some clinical implications in developing children.1
- Mechanism of action
The pyruvate kinase enzyme is an ATP-generating enzyme involved in the Embden–Meyerhof glycolytic pathway: it catalyzes the conversion of phosphoenolpyruvate to pyruvate in the final step of glycolysis, generating adenosine triphosphate (ATP), which is critical for cellular maintenance and survival. One of the four isoforms of pyruvate kinase - erythrocyte pyruvate kinase or PKR - is dedicated to red blood cells (RBCs). Compared to most human cells, RBCs lack the metabolic machinery required for aerobic metabolism of glucose and generation of ATP; thus, they rely on anaerobic glycolysis for ATP production. The deficiency of ATP due to glycolytic enzyme defects leads to shortened lifespan and premature destruction of RBCs in the form of chronic hemolytic anemia and ineffective erythropoiesis.1 Pyruvate kinase deficiency is a rare hereditary disorder affecting RBC glycolysis, caused by mutations in PKLR, the gene encoding the RBC (PKR) and liver-specific isoforms (PKL) of pyruvate kinase. Pyruvate kinase deficiency is associated with a build-up of 2,3-disphosphoglycerate (2,3-DPG), an upstream metabolite in glycolysis, and deficient ATP levels.4
Erythrocyte pyruvate kinase is an allosterically regulated homotetrameric enzyme 4 that is normally activated by fructose bisphosphate (FBP) in an allosteric fashion. Mitapivat is also an allosteric pyruvate kinase activator but binds to a different allosteric site from FBP on the PKR tetramer. This allows for the activation of both wild-type and mutant forms of erythrocyte pyruvate kinase, including those not induced by FBP.1,5 Upon binding to pyruvate kinase, mitapivat stabilizes the active tetrameric form of the enzyme and enhances its affinity for its substrate, phosphoenolpyruvate.3 Mitapivat upregulates erythrocyte pyruvate kinase activity, increases ATP production, and reduces levels of 2,3-DPG.1,5
Target Actions Organism APyruvate kinase PKLR activatorHumans UCytochrome P450 19A1 inhibitorHumans - Absorption
The absolute bioavailability of mitapivat after a single dose is approximately 73%. Mitapivat exposure increases dose-proportionally. Following twice-daily oral administration of mitapivat at the dose of 5 mg, 20 mg, and 50 mg, the mean (CV%) Cmax at steady state were 101.2 (17%) ng/mL, 389.9 (18%) ng/mL, and 935.2 (18%) ng/mL, respectively. The mean (CV%) AUC were 450.4 (28%) ng x h/mL, 1623.8 (28%) ng x h/mL, and 3591.4 (28%) ng x h/mL, respectively. The median Tmax values at steady state were 0.5 to 1.0 hour post-dose across the dose range of 5 mg to 50 mg twice daily.
In healthy subjects, a high-fat meal did not affect the drug exposure but reduced the rate of mitapivat absorption, with a 42% reduction in Cmax and a delay in Tmax of 2.3 hours when compared to dosing under fasted conditions.5
- Volume of distribution
The mean volume of distribution at steady state (Vss) was 42.5 L. 5
- Protein binding
Mitapivat is 97.7% bound to plasma proteins, with an RBC-to-plasma ratio of 0.37.5
- Metabolism
According to in vitro studies, mitapivat is primarily metabolized by CYP3A4.5 It is also a substrate of CYP1A2, CYP2C8, and CYP2C9.1 Following a single oral dose administration of 120 mg of radiolabeled mitapivat in healthy subjects, unchanged mitapivat was the major circulating component in plasma.5
- Route of elimination
Mitapivat is primary eliminated via hepatic metabolism.1 After a single oral administration of radiolabeled mitapivat in healthy subjects, the total recovery of administered radioactive dose was 89.2%. About 49.6% of radioactivity was recovered in the urine with 2.6% excreted as unchanged mitapivat. About 39.6% of radioactivity was recovered in the feces with less than 1% being the unchanged drug.5
- Half-life
In patients with pyruvate kinase deficiency receiving multiple doses of 5 mg mitapivat twice daily to 20 mg twice daily, the mean effective half-life (t1/2) of mitapivat ranged from 3 to 5 hours.5
- Clearance
Population pharmacokinetics derived median CL/F at steady state was 11.5, 12.7, and 14.4 L/h for the 5 mg twice daily, 20 mg twice daily, and 50 mg twice daily regimens, respectively.5
- Adverse Effects
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There is no information available regarding the LD50 and overdose profile of mitapivat.
- 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 increased when combined with Mitapivat. Abametapir The serum concentration of Mitapivat can be increased when it is combined with Abametapir. Abemaciclib The metabolism of Abemaciclib can be increased when combined with Mitapivat. Acalabrutinib The metabolism of Acalabrutinib can be increased when combined with Mitapivat. Acarbose The therapeutic efficacy of Acarbose can be increased when used in combination with Mitapivat. - Food Interactions
- Take with or without food. Food has a negligible effect on the exposure of mitapivat, but may reduce the rate of drug absorption, Cmax, and Tmax.
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 Mitapivat sulfate N4JTA67V3O Not Available Not applicable - Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Pyrukynd Tablet, film coated 5 mg/1 Oral Agios Pharmaceuticals, Inc. 2022-02-18 Not applicable US 
Pyrukynd Tablet, film coated 5 mg/1 Oral Agios Pharmaceuticals, Inc. 2022-02-18 Not applicable US Pyrukynd Tablet, film coated 20 mg Oral Agios Netherlands B.V. 2023-02-08 Not applicable EU 
Pyrukynd Tablet, film coated 5 mg Oral Agios Netherlands B.V. 2023-02-08 Not applicable EU Pyrukynd Tablet, film coated 50 mg/1 Oral Agios Pharmaceuticals, Inc. 2022-02-18 Not applicable US - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Pyrukynd Mitapivat (20 mg/1) + Mitapivat (50 mg/1) Kit; Tablet, film coated Oral Agios Pharmaceuticals, Inc. 2022-02-18 Not applicable US Pyrukynd Mitapivat (5 mg/1) + Mitapivat (20 mg/1) Kit; Tablet, film coated Oral Agios Pharmaceuticals, Inc. 2022-02-18 Not applicable US Pyrukynd Mitapivat (20 mg/1) + Mitapivat (50 mg/1) Kit; Tablet, film coated Oral Agios Pharmaceuticals, Inc. 2022-02-18 Not applicable US Pyrukynd Mitapivat (5 mg/1) + Mitapivat (20 mg/1) Kit; Tablet, film coated Oral Agios Pharmaceuticals, Inc. 2022-02-18 Not applicable US
Categories
- ATC Codes
- G01AE10 — Combinations of sulfonamides
- G01AE — Sulfonamides
- G01A — ANTIINFECTIVES AND ANTISEPTICS, EXCL. COMBINATIONS WITH CORTICOSTEROIDS
- G01 — GYNECOLOGICAL ANTIINFECTIVES AND ANTISEPTICS
- G — GENITO URINARY SYSTEM AND SEX HORMONES
- Drug Categories
- Anemia, Hemolytic, Congenital, drug therapy
- Blood and Blood Forming Organs
- Cytochrome P-450 CYP1A2 Substrates
- Cytochrome P-450 CYP2B6 Inducers
- Cytochrome P-450 CYP2B6 Inducers (strength unknown)
- Cytochrome P-450 CYP2C19 Inducers
- Cytochrome P-450 CYP2C19 Inducers (strength unknown)
- Cytochrome P-450 CYP2C8 Inducers
- Cytochrome P-450 CYP2C8 Inducers (strength unknown)
- Cytochrome P-450 CYP2C8 Substrates
- Cytochrome P-450 CYP2C9 Inducers
- Cytochrome P-450 CYP2C9 Inducers (strength unknown)
- Cytochrome P-450 CYP2C9 Substrates
- 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 Enzyme Inducers
- Cytochrome P-450 Substrates
- Enzyme Activators
- Genito Urinary System and Sex Hormones
- Gynecological Antiinfectives and Antiseptics
- Heterocyclic Compounds, Fused-Ring
- P-glycoprotein inhibitors
- P-glycoprotein substrates
- Pyruvate Kinase Activator
- Sulfonamides
- Sulfones
- UGT1A1 Inducers
- Classification
- Not classified
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- 2WTV10SIKH
- CAS number
- 1260075-17-9
- InChI Key
- XAYGBKHKBBXDAK-UHFFFAOYSA-N
- InChI
- InChI=1S/C24H26N4O3S/c29-24(28-15-13-27(14-16-28)17-18-6-7-18)20-8-10-21(11-9-20)26-32(30,31)22-5-1-3-19-4-2-12-25-23(19)22/h1-5,8-12,18,26H,6-7,13-17H2
- IUPAC Name
- N-{4-[4-(cyclopropylmethyl)piperazine-1-carbonyl]phenyl}quinoline-8-sulfonamide
- SMILES
- O=C(N1CCN(CC2CC2)CC1)C1=CC=C(NS(=O)(=O)C2=CC=CC3=C2N=CC=C3)C=C1
References
- General References
- Al-Samkari H, van Beers EJ: Mitapivat, a novel pyruvate kinase activator, for the treatment of hereditary hemolytic anemias. Ther Adv Hematol. 2021 Dec 21;12:20406207211066070. doi: 10.1177/20406207211066070. eCollection 2021. [Article]
- Perez EA, Weilbaecher K: Aromatase inhibitors and bone loss. Oncology (Williston Park). 2006 Aug;20(9):1029-39; discussion 1039-40, 1042, 1048. [Article]
- Matte A, Federti E, Kung C, Kosinski PA, Narayanaswamy R, Russo R, Federico G, Carlomagno F, Desbats MA, Salviati L, Leboeuf C, Valenti MT, Turrini F, Janin A, Yu S, Beneduce E, Ronseaux S, Iatcenko I, Dang L, Ganz T, Jung CL, Iolascon A, Brugnara C, De Franceschi L: The pyruvate kinase activator mitapivat reduces hemolysis and improves anemia in a beta-thalassemia mouse model. J Clin Invest. 2021 May 17;131(10). pii: 144206. doi: 10.1172/JCI144206. [Article]
- Rab MAE, Van Oirschot BA, Kosinski PA, Hixon J, Johnson K, Chubukov V, Dang L, Pasterkamp G, Van Straaten S, Van Solinge WW, Van Beers EJ, Kung C, Van Wijk R: AG-348 (Mitapivat), an allosteric activator of red blood cell pyruvate kinase, increases enzymatic activity, protein stability, and ATP levels over a broad range of PKLR genotypes. Haematologica. 2021 Jan 1;106(1):238-249. doi: 10.3324/haematol.2019.238865. [Article]
- FDA Approved Drug Products: PYRUKYND (mitapivat) tablets, for oral use [Link]
- GlobeNewsWire: Agios Announces FDA Approval of PYRUKYND® (mitapivat) as First Disease-Modifying Therapy for Hemolytic Anemia in Adults with Pyruvate Kinase Deficiency [Link]
- External Links
- ChemSpider
- 29763395
- 2594468
- ChEMBL
- CHEMBL4299940
- ZINC
- ZINC000140430983
- Wikipedia
- Mitapivat
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 Enrolling by Invitation Treatment Hemolytic Anemia / Pyruvate Kinase Deficiency 1 3 Active Not Recruiting Treatment Non-Transfusion-dependent Alpha-Thalassemia / Non-Transfusion-dependent Beta-Thalassemia 1 3 Active Not Recruiting Treatment Pediatric Hemolytic Anemia / Pediatric Pyruvate Kinase Deficiency 1 3 Active Not Recruiting Treatment Pyruvate Kinase Deficiency 1 3 Active Not Recruiting Treatment Transfusion-dependent Alpha-Thalassemia / Transfusion-dependent Beta-Thalassemia 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Kit; tablet, film coated Oral Tablet, film coated Oral 20 mg Tablet, film coated Oral 20 mg/1 Tablet, film coated Oral 5 mg/1 Tablet, film coated Oral 5 mg Tablet, film coated Oral 50 mg/1 Tablet, film coated Oral 50 mg - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US9193701 No 2015-11-24 2032-10-26 US US9682080 No 2017-06-20 2032-05-03 US US9980961 No 2018-05-29 2032-05-03 US US10632114 No 2020-04-28 2032-05-03 US US11234976 No 2018-10-11 2038-10-11 US US11254652 No 2018-11-21 2038-11-21 US US8785450 No 2014-07-22 2031-02-24 US USRE49582 No 2011-02-24 2031-02-24 US US11793806 No 2013-04-12 2033-04-12 US
Properties
- State
- Solid
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source Water Solubility 0.0329 mg/mL ALOGPS logP 3.08 ALOGPS logP 1.62 Chemaxon logS -4.1 ALOGPS pKa (Strongest Acidic) 6.79 Chemaxon pKa (Strongest Basic) 7.64 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 5 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 82.61 Å2 Chemaxon Rotatable Bond Count 5 Chemaxon Refractivity 123.68 m3·mol-1 Chemaxon Polarizability 46.21 Å3 Chemaxon Number of Rings 5 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No 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 splash10-0udi-0000900000-44e9fc96b38c7f7eee65 Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-0002-0004900000-c7339cb6ff47f3d15b20 Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-0005-0900700000-35e68cd5808584538551 Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-0udi-2004900000-149d8bd2ea12f1a20002 Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-0100-0918600000-f5e04c5e386e67033649 Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-00l6-0913200000-a18b3886f784d0c6a54b Predicted 1H NMR Spectrum 1D NMR Not Applicable Predicted 13C NMR Spectrum 1D NMR Not Applicable - Chromatographic Properties
Collision Cross Sections (CCS)
Not Available
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Activator
- General Function
- Pyruvate kinase activity
- Specific Function
- Plays a key role in glycolysis.
- Gene Name
- PKLR
- Uniprot ID
- P30613
- Uniprot Name
- Pyruvate kinase PKLR
- Molecular Weight
- 61829.575 Da
References
- Al-Samkari H, van Beers EJ: Mitapivat, a novel pyruvate kinase activator, for the treatment of hereditary hemolytic anemias. Ther Adv Hematol. 2021 Dec 21;12:20406207211066070. doi: 10.1177/20406207211066070. eCollection 2021. [Article]
- Rab MAE, Van Oirschot BA, Kosinski PA, Hixon J, Johnson K, Chubukov V, Dang L, Pasterkamp G, Van Straaten S, Van Solinge WW, Van Beers EJ, Kung C, Van Wijk R: AG-348 (Mitapivat), an allosteric activator of red blood cell pyruvate kinase, increases enzymatic activity, protein stability, and ATP levels over a broad range of PKLR genotypes. Haematologica. 2021 Jan 1;106(1):238-249. doi: 10.3324/haematol.2019.238865. [Article]
- FDA Approved Drug Products: PYRUKYND (mitapivat) tablets, for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Oxygen binding
- Specific Function
- Catalyzes the formation of aromatic C18 estrogens from C19 androgens.
- Gene Name
- CYP19A1
- Uniprot ID
- P11511
- Uniprot Name
- Aromatase
- Molecular Weight
- 57882.48 Da
References
- Al-Samkari H, van Beers EJ: Mitapivat, a novel pyruvate kinase activator, for the treatment of hereditary hemolytic anemias. Ther Adv Hematol. 2021 Dec 21;12:20406207211066070. doi: 10.1177/20406207211066070. eCollection 2021. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- 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
- FDA Approved Drug Products: PYRUKYND (mitapivat) tablets, for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- 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: PYRUKYND (mitapivat) tablets, for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- SubstrateInducer
- 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
- Al-Samkari H, van Beers EJ: Mitapivat, a novel pyruvate kinase activator, for the treatment of hereditary hemolytic anemias. Ther Adv Hematol. 2021 Dec 21;12:20406207211066070. doi: 10.1177/20406207211066070. eCollection 2021. [Article]
- FDA Approved Drug Products: PYRUKYND (mitapivat) tablets, for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- SubstrateInducer
- 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
- Al-Samkari H, van Beers EJ: Mitapivat, a novel pyruvate kinase activator, for the treatment of hereditary hemolytic anemias. Ther Adv Hematol. 2021 Dec 21;12:20406207211066070. doi: 10.1177/20406207211066070. eCollection 2021. [Article]
- FDA Approved Drug Products: PYRUKYND (mitapivat) tablets, for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inducer
- 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: PYRUKYND (mitapivat) tablets, for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inducer
- 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: PYRUKYND (mitapivat) tablets, for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
- 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
- CYP1A2
- Uniprot ID
- P05177
- Uniprot Name
- Cytochrome P450 1A2
- Molecular Weight
- 58293.76 Da
References
- Al-Samkari H, van Beers EJ: Mitapivat, a novel pyruvate kinase activator, for the treatment of hereditary hemolytic anemias. Ther Adv Hematol. 2021 Dec 21;12:20406207211066070. doi: 10.1177/20406207211066070. eCollection 2021. [Article]
Transporters
- 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: PYRUKYND (mitapivat) tablets, for oral use [Link]
Drug created at December 15, 2020 18:16 / Updated at March 08, 2022 12:10