Alpelisib

Identification

Brand Names
Piqray 300 Mg Daily Dose, Vijoice 50 Mg 28 Day
Generic Name
Alpelisib
DrugBank Accession Number
DB12015
Background

Alpelisib is a phosphatidylinositol 3-kinase (PI3K) inhibitor with potent antitumor activity. It works by selectively inhibiting class I PI3K p110α 2, which is the catalytic subunit of PI3K, a lipid kinase that plays a role in various biological processes, including proliferation, survival, differentiation, and metabolism. Alpelisib was designed to target this enzyme that appears to be mutated at a rate of nearly 30% in human cancers, leading to hyperactivation.3

There are several isoform-specific PI3K inhibitors that are under clinical development or currently approved, such as idelalisib used for chronic lymphocytic leukemia (CLL).3 Approved by the FDA in May 2019, alpelisib is the first approved PI3K inhibitor indicated for the treatment of hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative, PIK3CA-mutated, advanced or metastatic breast cancer in combination with fulvestrant for postmenopausal women and male patients. To initiate alpelisib therapy, it is required that the presence of a PIK3CA mutation in the tissue and/or liquid biopsy sample collection should be confirmed via FDA-approved diagnostic tests. Alpelisib is marketed under the trade name Piqray and is available as oral tablets. Studies evaluating the therapeutic effectiveness of alpelisib in other cancers, such as ovarian cancer 1 and colorectal cancer 2, are under ongoing investigations.

Alpelisib was granted FDA approval on 24 May 2019.7 In April 2022, the FDA granted the use of alpelisib in the treatment of PIK3CA-Related Overgrowth Spectrum (PROS) in adults and children who require systemic therapy.8

Type
Small Molecule
Groups
Approved, Investigational
Structure
Weight
Average: 441.47
Monoisotopic: 441.144630278
Chemical Formula
C19H22F3N5O2S
Synonyms
  • Alpelisib
External IDs
  • BYL 719
  • BYL-719
  • BYL719
  • NVP-BYL719

Pharmacology

Indication

Alpelisib is indicated in combination with fulvestrant to treat postmenopausal women, and men, with advanced or metastatic breast cancer. This cancer must be hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative, and PIK3CA­ mutated. The cancer must be detected by an FDA-approved test following progression on or after an endocrine-based regimen.7

Alpelisib is also used to treat adult and pediatric patients two years of age and older with severe manifestations of PIK3CA-Related Overgrowth Spectrum (PROS) who require systemic therapy. This indication is approved under accelerated approval based on response rate and duration of response. Continued approval for this indication may be contingent upon verification and description of clinical benefit in a confirmatory trial(s).8

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Treatment ofPik3ca-related overgrowth spectrum (pros)•••••••••••••••••• •••••••• ••••••••• ••••••• •••••••• •••••••••••••
Used in combination to treatAdvanced hr + her2 - breast cancerRegimen in combination with: Fulvestrant (DB00947)•••••••••••••••••• •••••••••••••••••••• •••• ••••••••• ••••••• ••••••••••• ••••• ••••••••• ••••• •••••••••••••
Used in combination to treatMetastatic hr + her2 - breast cancerRegimen in combination with: Fulvestrant (DB00947)•••••••••••••••••• ••••••••••••••••••••• ••••••••••• ••••• ••••••••• ••••• •••••••• •••••• •••• ••••••••••••••
Contraindications & Blackbox Warnings
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Pharmacodynamics

Alpelisib does not prolong the QTcF interval.7 Patients taking alpelisib experience a dose dependent benefit from treatment with a 51% advantage of a 200mg daily dose over a 100mg dose and a 22% advantage of 300mg once daily over 150mg twice daily.6 This suggests patients requiring a lower dose may benefit from twice daily dosing.6

Mechanism of action

Phosphatidylinositol-3-kinase-α (PI3Kα) is responsible for cell proliferation in response to growth factor-tyrosine kinase pathway activation.3 In some cancers PI3Kα's p110α catalytic subunit is mutated making it hyperactive.3 Alpelisib inhibits (PI3K), with the highest specificity for PI3Kα.7

TargetActionsOrganism
APhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform
inhibitor
Humans
Absorption

Alpelisib reached a peak concentration in plasma of 1320±912ng/mL after 2 hours.4 Alpelisib has an AUClast of 11,100±3760h ng/mL and an AUCINF of 11,100±3770h ng/mL.4 A large, high fat meal increases the AUC by 73% and Cmax by 84% while a small, low fat meal increases the AUC by 77% and Cmax by 145%.7

Volume of distribution

The apparent volume of distribution at steady state is 114L.7

Protein binding

Alpelisib is 89% protein bound.7

Metabolism

Alpelisib is metabolized by hydrolysis reactions to form the primary metabolite. It is also metabolized by CYP3A4.7 The full metabolism of Alpelisib has yet to be determined but a series of reactions have been proposed.4,5 The main metabolic reaction is the substitution of an amine group on alpelisib for a hydroxyl group to form a metabolite known as M44,5 or BZG791.7 Alpelisib can also be glucuronidated to form the M1 and M12 metabolites.4,5

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Route of elimination

36% of an oral dose is eliminated as unchanged drug in the feces and 32% as the primary metabolite BZG791 in the feces. About 2% of an oral dose is eliminated in the urine as unchanged drug and 7.1% as the primary metabolite BZG791. In total 81% of an oral dose is eliminated in the feces and 14% is eliminated in the urine.7

Half-life

The mean half life of alprelisib is 8 to 9 hours.7

Clearance

The mean apparent oral clearance was 39.0L/h.4 The predicted clearance is 9.2L/hr under fed conditions.7

Adverse Effects
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Toxicity

Patients experiencing an overdose may present with hyperglycemia, nausea, asthenia, and rash. There is no antidote for an overdose of alpelisib so patients should be treated symptomatically.7

Data regarding an LD50 is not readily available.9 In clinical trials, patients were given doses of up to 450mg once daily.7

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.
DrugInteraction
AbametapirThe serum concentration of Alpelisib can be increased when it is combined with Abametapir.
AbataceptThe metabolism of Alpelisib can be increased when combined with Abatacept.
AbemaciclibThe serum concentration of Alpelisib can be increased when it is combined with Abemaciclib.
AbrocitinibThe serum concentration of Abrocitinib can be decreased when it is combined with Alpelisib.
AcalabrutinibThe metabolism of Acalabrutinib can be increased when combined with Alpelisib.
Food Interactions
  • Exercise caution with St. John's Wort. This herb induces CYP3A metabolism and may reduce serum levels of alpelisib.
  • Take at the same time every day.
  • Take with food. Food does not significantly affect the AUC of alpelisib.

Products

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Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
PiqrayTablet, film coated200 mgOralNovartis Europharm Limited2020-12-16Not applicableEU flag
PiqrayTablet, film coated150 mgOralNovartis Europharm Limited2020-12-16Not applicableEU flag
PiqrayTablet200 mgOralNovartis2020-06-29Not applicableCanada flag
PiqrayTablet200 mg/1OralNovartis Pharmaceuticals Corporation2019-05-24Not applicableUS flag
PiqrayTablet, film coated200 mgOralNovartis Europharm Limited2020-12-16Not applicableEU flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
PIQRAYAlpelisib (200 MG) + Alpelisib (50 MG)Kit; Tablet, film coatedOralNovartis Europharm Limited2020-12-05Not applicableItaly flag
PIQRAYAlpelisib (200 MG) + Alpelisib (50 MG)Kit; Tablet, film coatedOralNovartis Europharm Limited2020-12-05Not applicableItaly flag
PiqrayAlpelisib (200 mg/1) + Alpelisib (50 mg/1)Kit; TabletOralNovartis Pharmaceuticals Corporation2019-05-24Not applicableUS flag
PIQRAYAlpelisib (200 MG) + Alpelisib (50 MG)Kit; Tablet, film coatedOralNovartis Europharm Limited2020-12-05Not applicableItaly flag
PIQRAYAlpelisib (200 MG) + Alpelisib (50 MG)Kit; Tablet, film coatedOralNovartis Europharm Limited2020-12-05Not applicableItaly flag

Categories

ATC Codes
L01EM03 — Alpelisib
Drug Categories
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 / Pyrrolidinecarboxamides / 2,4,5-trisubstituted thiazoles / Pyridines and derivatives / Heteroaromatic compounds / Ureas / Primary carboxylic acid amides / Azacyclic compounds / Organopnictogen compounds / Organonitrogen compounds
show 5 more
Substituents
2,4,5-trisubstituted 1,3-thiazole / Alkyl fluoride / Alkyl halide / Alpha-amino acid amide / Aromatic heteromonocyclic compound / Azacycle / Azole / Carbonic acid derivative / Carbonyl group / Carboxamide group
show 20 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
Not Available
Affected organisms
Not Available

Chemical Identifiers

UNII
08W5N2C97Q
CAS number
1217486-61-7
InChI Key
STUWGJZDJHPWGZ-LBPRGKRZSA-N
InChI
InChI=1S/C19H22F3N5O2S/c1-10-14(11-6-7-24-13(9-11)18(2,3)19(20,21)22)30-16(25-10)26-17(29)27-8-4-5-12(27)15(23)28/h6-7,9,12H,4-5,8H2,1-3H3,(H2,23,28)(H,25,26,29)/t12-/m0/s1
IUPAC Name
(2S)-N1-{4-methyl-5-[2-(1,1,1-trifluoro-2-methylpropan-2-yl)pyridin-4-yl]-1,3-thiazol-2-yl}pyrrolidine-1,2-dicarboxamide
SMILES
CC1=C(SC(NC(=O)N2CCC[C@H]2C(N)=O)=N1)C1=CC(=NC=C1)C(C)(C)C(F)(F)F

References

General References
  1. Konstantinopoulos PA, Barry WT, Birrer M, Westin SN, Cadoo KA, Shapiro GI, Mayer EL, O'Cearbhaill RE, Coleman RL, Kochupurakkal B, Whalen C, Curtis J, Farooq S, Luo W, Eismann J, Buss MK, Aghajanian C, Mills GB, Palakurthi S, Kirschmeier P, Liu J, Cantley LC, Kaufmann SH, Swisher EM, D'Andrea AD, Winer E, Wulf GM, Matulonis UA: Olaparib and alpha-specific PI3K inhibitor alpelisib for patients with epithelial ovarian cancer: a dose-escalation and dose-expansion phase 1b trial. Lancet Oncol. 2019 Apr;20(4):570-580. doi: 10.1016/S1470-2045(18)30905-7. Epub 2019 Mar 14. [Article]
  2. Rodon J, Curigliano G, Delord JP, Harb W, Azaro A, Han Y, Wilke C, Donnet V, Sellami D, Beck T: A Phase Ib, open-label, dose-finding study of alpelisib in combination with paclitaxel in patients with advanced solid tumors. Oncotarget. 2018 Aug 3;9(60):31709-31718. doi: 10.18632/oncotarget.25854. eCollection 2018 Aug 3. [Article]
  3. Yang X, Zhang X, Huang M, Song K, Li X, Huang M, Meng L, Zhang J: New Insights into PI3K Inhibitor Design using X-ray Structures of PI3Kalpha Complexed with a Potent Lead Compound. Sci Rep. 2017 Nov 6;7(1):14572. doi: 10.1038/s41598-017-15260-5. [Article]
  4. James A, Blumenstein L, Glaenzel U, Jin Y, Demailly A, Jakab A, Hansen R, Hazell K, Mehta A, Trandafir L, Swart P: Absorption, distribution, metabolism, and excretion of [(14)C]BYL719 (alpelisib) in healthy male volunteers. Cancer Chemother Pharmacol. 2015 Oct;76(4):751-60. doi: 10.1007/s00280-015-2842-4. Epub 2015 Aug 8. [Article]
  5. James AD, Marvalin C, Luneau A, Meissner A, Camenisch G: Comparison of (19)F NMR and (14)C Measurements for the Assessment of ADME of BYL719 (Alpelisib) in Humans. Drug Metab Dispos. 2017 Aug;45(8):900-907. doi: 10.1124/dmd.117.075424. Epub 2017 May 31. [Article]
  6. De Buck SS, Jakab A, Boehm M, Bootle D, Juric D, Quadt C, Goggin TK: Population pharmacokinetics and pharmacodynamics of BYL719, a phosphoinositide 3-kinase antagonist, in adult patients with advanced solid malignancies. Br J Clin Pharmacol. 2014 Sep;78(3):543-55. doi: 10.1111/bcp.12378. [Article]
  7. FDA Approved Drug Products: PIQRAY (alpelisib) tablets, for oral use [Link]
  8. FDA Approved Drug Products: VIJOICE (alpelisib) tablets, for oral use [Link]
  9. Cayman Chemical: Alpelisib MSDS [Link]
  10. FDA Approved Drug Products: PIQRAY (alpelisib) tablets, for oral use [Link]
Human Metabolome Database
HMDB0304878
PubChem Compound
56649450
PubChem Substance
347828332
ChemSpider
28424123
BindingDB
50436459
RxNav
2169285
ChEBI
93752
ChEMBL
CHEMBL2396661
ZINC
ZINC000068198368
PDBe Ligand
1LT
Wikipedia
Phosphoinositide_3-kinase_inhibitor
PDB Entries
4jps / 7myo / 7pg6 / 8gua / 8gub / 8gud

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4RecruitingTreatmentAdvanced Breast Cancer1
3Active Not RecruitingTreatmentAdvanced HER2+Breast Cancer1
3Active Not RecruitingTreatmentOvarian Cancer1
3Active Not RecruitingTreatmentTriple-Negative Breast Neoplasm1
3CompletedTreatmentBreast Cancer2

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Kit; tabletOral
Kit; tablet, film coatedOral
TabletOral150 mg
TabletOral150 mg/1
TabletOral200 mg/1
TabletOral200 mg
TabletOral50 mg
TabletOral500.000 mg
Tablet, film coatedOral200 mg
Tablet, film coatedOral150 mg
Tablet, film coatedOral
TabletOral125 mg/1
TabletOral50 mg/1
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US8227462No2012-07-242030-09-28US flag
US8476268No2013-07-022029-09-10US flag

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.00528 mg/mLALOGPS
logP2.76ALOGPS
logP2.81Chemaxon
logS-4.9ALOGPS
pKa (Strongest Acidic)7.79Chemaxon
pKa (Strongest Basic)2.81Chemaxon
Physiological Charge0Chemaxon
Hydrogen Acceptor Count4Chemaxon
Hydrogen Donor Count2Chemaxon
Polar Surface Area101.21 Å2Chemaxon
Rotatable Bond Count5Chemaxon
Refractivity105.85 m3·mol-1Chemaxon
Polarizability42.75 Å3Chemaxon
Number of Rings3Chemaxon
Bioavailability1Chemaxon
Rule of FiveYesChemaxon
Ghose FilterYesChemaxon
Veber's RuleNoChemaxon
MDDR-like RuleNoChemaxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSsplash10-0f96-0004900000-d9dc3aa20948b9a6341e
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSsplash10-0ukc-0407900000-c01635164825876b9778
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSsplash10-0006-7504900000-aaff4ff6533307379394
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSsplash10-0006-9210000000-e538b563b62bda8f215c
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSsplash10-05fs-9002000000-0918a6fd14b0f97edafe
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSsplash10-0006-9023000000-9b674d4080056f5c6da1
Predicted 1H NMR Spectrum1D NMRNot Applicable
Predicted 13C NMR Spectrum1D NMRNot Applicable
Chromatographic Properties
Collision Cross Sections (CCS)
AdductCCS Value (Å2)Source typeSource
[M-H]-191.60745
predicted
DeepCCS 1.0 (2019)
[M+H]+193.96547
predicted
DeepCCS 1.0 (2019)
[M+Na]+200.15466
predicted
DeepCCS 1.0 (2019)

Targets

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insights and accelerate drug research.
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Use our structured and evidence-based datasets to unlock new insights and accelerate drug research.
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Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
Protein serine/threonine kinase activity
Specific Function
Phosphoinositide-3-kinase (PI3K) that phosphorylates PtdIns (Phosphatidylinositol), PtdIns4P (Phosphatidylinositol 4-phosphate) and PtdIns(4,5)P2 (Phosphatidylinositol 4,5-bisphosphate) to generate...
Gene Name
PIK3CA
Uniprot ID
P42336
Uniprot Name
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform
Molecular Weight
124283.025 Da
References
  1. Chen IC, Hsiao LP, Huang IW, Yu HC, Yeh LC, Lin CH, Wei-Wu Chen T, Cheng AL, Lu YS: Phosphatidylinositol-3 Kinase Inhibitors, Buparlisib and Alpelisib, Sensitize Estrogen Receptor-positive Breast Cancer Cells to Tamoxifen. Sci Rep. 2017 Aug 29;7(1):9842. doi: 10.1038/s41598-017-10555-z. [Article]
  2. Yang X, Zhang X, Huang M, Song K, Li X, Huang M, Meng L, Zhang J: New Insights into PI3K Inhibitor Design using X-ray Structures of PI3Kalpha Complexed with a Potent Lead Compound. Sci Rep. 2017 Nov 6;7(1):14572. doi: 10.1038/s41598-017-15260-5. [Article]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
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
  1. James AD, Marvalin C, Luneau A, Meissner A, Camenisch G: Comparison of (19)F NMR and (14)C Measurements for the Assessment of ADME of BYL719 (Alpelisib) in Humans. Drug Metab Dispos. 2017 Aug;45(8):900-907. doi: 10.1124/dmd.117.075424. Epub 2017 May 31. [Article]
  2. James A, Blumenstein L, Glaenzel U, Jin Y, Demailly A, Jakab A, Hansen R, Hazell K, Mehta A, Trandafir L, Swart P: Absorption, distribution, metabolism, and excretion of [(14)C]BYL719 (alpelisib) in healthy male volunteers. Cancer Chemother Pharmacol. 2015 Oct;76(4):751-60. doi: 10.1007/s00280-015-2842-4. Epub 2015 Aug 8. [Article]
  3. New Mexico Cancer Alliance: Compassionate Use of Alpelisib [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
CYP2C9
Uniprot ID
P11712
Uniprot Name
Cytochrome P450 2C9
Molecular Weight
55627.365 Da
References
  1. Rewcastle GW, Kolekar S, Buchanan CM, Gamage SA, Giddens AC, Tsang KY, Kendall JD, Singh R, Lee WJ, Smith GC, Han W, Matthews DJ, Denny WA, Shepherd PR, Jamieson SMF: Biological characterization of SN32976, a selective inhibitor of PI3K and mTOR with preferential activity to PI3Kalpha, in comparison to established pan PI3K inhibitors. Oncotarget. 2017 Jul 18;8(29):47725-47740. doi: 10.18632/oncotarget.17730. [Article]
  2. New Mexico Cancer Alliance: Compassionate Use of Alpelisib [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2C8
Uniprot ID
P10632
Uniprot Name
Cytochrome P450 2C8
Molecular Weight
55824.275 Da
References
  1. New Mexico Cancer Alliance: Compassionate Use of Alpelisib [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
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
  1. New Mexico Cancer Alliance: Compassionate Use of Alpelisib [Link]

Transporters

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
References
  1. New Mexico Cancer Alliance: Compassionate Use of Alpelisib [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
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
  1. FDA Approved Drug Products: PIQRAY (alpelisib) tablets, for oral use [Link]

Drug created at October 20, 2016 21:11 / Updated at March 18, 2024 19:36