Leniolisib
Identification
- Summary
Leniolisib is a phosphoinositide 3-kinase-delta inhibitor that is used to treat activated phosphoinositide 3-kinase delta syndrome.
- Brand Names
- Joenja
- Generic Name
- Leniolisib
- DrugBank Accession Number
- DB16217
- Background
Leniolisib is a potent and selective inhibitor of phosphoinositide 3-kinase δ (PI3Kδ). The FDA approved leniolisib on March 24, 2023, making it the first treatment for activated phosphoinositide 3-kinase delta syndrome (APDS).10 APDS is a primary immunodeficiency caused by mutations in genes encoding the PI3Kδ, thereby increasing the activity of PI3Kδ, causing immune dysfunction, and elevating susceptibility to infections.1,2 Leniolisib works to inhibit hyperactive PI3Kδ.9 Investigations for using leniolisib in primary Sjögren’s syndrome are ongoing.3
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
- Weight
- Average: 450.466
Monoisotopic: 450.199108558 - Chemical Formula
- C21H25F3N6O2
- Synonyms
- Cdz-173 free base
- Cdz173 free base
- Leniolisib
- External IDs
- CDZ-173-NX
- CDZ173
- CDZ173-NX
Pharmacology
- Indication
Leniolisib is indicated for the treatment of activated phosphoinositide 3-kinase delta (PI3Kδ) syndrome (APDS) in adult and pediatric patients 12 years of age and older.9
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Treatment of Activated pi3 kinase delta syndrome •••••••••••• ••••••••••• ••••• - Contraindications & Blackbox Warnings
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- Pharmacodynamics
Leniolisib works to block aberrant PI3Kδ-dependent signalling pathways of immune cells, such as B and T cells, neutrophils, monocytes, basophils, plasmocytoid dendritic cells, and mast cells.3 In vitro, leniolisib dose-dependently suppresses the PI3Kδ pathway hyperactivation in cell lines overexpressing p110δ mutants and in primary immune cells from patients with APDS.2 Ex vivo pharmacodynamics of leniolisib in the proportion of phosphorylated Akt (pAkt)- positive B cells were assessed intra-individually at 10, 30, and 70 mg twice daily for four weeks at each dose level in patients with APDS. Within the explored dose range, higher leniolisib plasma concentrations were generally associated with a higher reduction of pAkt-positive B cells. Higher doses were associated with a slightly higher peak and more sustained reduction. Treatment with leniolisib 70 mg twice a day at a steady state is estimated to produce a time-averaged reduction of pAkt-positive B cells by approximately 80%.9
- Mechanism of action
Phosphoinositide-3-kinase δ (PI3Kδ) is a lipid kinase activated downstream of tyrosine kinase receptors and G-protein–coupled receptors in immune cells.1,3,8 It mediates the PI3K/AKT pathway, which is involved in cell proliferation, growth, and survival.6,7 A heterodimer made up of a regulatory subunit (p85α) and a catalytic subunit (p110δ), PI3Kδ is primarily expressed on hematopoietic cells such as lymphocytes and myeloid cells. It converts phosphatidylinositol-4,5-bisphosphate (PIP2) to phosphatidylinositol-3,4,5-trisphosphate (PIP3), a signalling molecule that downstream proteins like the AKT kinase, which activate mammalian target of rapamycin (mTOR) complex I and inhibit FOXO family of transcription factors.1,2 APDS is associated with gain-of-function variants in the gene encoding p110δ or loss of function variants in the gene encoding p85α, each causing hyperactivity of PI3K-delta, reduced T cell function, lymphadenopathy, and immunodeficiency.1,9
Leniolisib inhibits PI3Kδ by blocking the active binding site in the p110δ subunit.2 In cell-free isolated enzyme assays, the selectivity was higher for PI3K-delta over PI3K-alpha (28-fold), PI3K-beta (43-fold), and PI3K-gamma (257-fold), as well as the broader kinome. In cell-based assays, leniolisib reduced pAKT pathway activity and inhibited proliferation and activation of B and T cell subsets. Leniolisib inhibits the signalling pathways that lead to increased production of PIP3, hyperactivity of the downstream mTOR/AKT pathway, and the dysregulation of B and T cells.9
Target Actions Organism APhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform inhibitorHumans - Absorption
The systemic drug exposure (AUC and Cmax) of leniolisib increases dose proportionally. During twice daily dosing approximately 12 hours apart, leniolisib accumulates approximately 1.4-fold (range of 1.0 to 2.2) in achieving steady-state. Steady-state drug concentrations can be expected to be reached after approximately two to three days. The Tmax is about one hour. Food has negligible effects on the systemic exposure of leniolisib.9
- Volume of distribution
The systemic decay in leniolisib plasma concentration over time is bi-exponential, indicating a distribution delay toward peripheral tissues. The volume of distribution of leniolisib is estimated to be 28.5 L in patients with APDS.9
- Protein binding
Leniolisib is 94.5% bound to plasma proteins.9
- Metabolism
About 60% of leniolisib is metabolized by the liver. Leniolisib undergoes oxidative metabolism, which is primarily mediated by CYP3A4 (94.5%), as well as CYP3A5 (3.5%), CYP1A2 (0.7%) and CYP2D6 (0.7%) to a minor extent.4,9 Few metabolites of leniolisib have been characterized in one study; however, no metabolites were abundant in plasma relative to the parent drug. Other metabolic pathways include dealkylation, demethylation, and hydroxylation.5
Other suggested excretion routes include intestinal secretion by BCRP and CYP1A1-mediated extrahepatic metabolism.4,9
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- Route of elimination
The mean recovery of total 14C-radioactivity following a single oral dose of 70 mg 14C-leniolisib was 92.5% following 168 hours post-dose. About 67% and 25.5% of the recovered dose were in feces and urine, respectively. Of the recovered dose in urine, 6.32% was in unchanged parent drug form and the predominant drug-related material.9
- Half-life
The effective half-life is approximately seven hours. The apparent terminal elimination half-life is approximately 10 hours.9
- Clearance
In one study, healthy volunteers received leniolisib single ascending doses up to 400 mg and multiple ascending doses up to 140 mg twice daily for 14 days. Oral drug clearance from plasma (CL/F) was 4 L/h.4
- Adverse Effects
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- Toxicity
No information on the LD50 of leniolisib is available. If overdosage occurs, monitor the patient for any signs or symptoms of adverse reactions. Treatment of overdose with leniolisib consists of general supportive measures, including monitoring of vital signs as well as observation of the clinical status of the patient.9
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbemaciclib The excretion of Abemaciclib can be decreased when combined with Leniolisib. Acenocoumarol The metabolism of Acenocoumarol can be decreased when combined with Leniolisib. Acetaminophen The metabolism of Acetaminophen can be decreased when combined with Leniolisib. Acyclovir The metabolism of Acyclovir can be decreased when combined with Leniolisib. Adenovirus type 7 vaccine live The therapeutic efficacy of Adenovirus type 7 vaccine live can be decreased when used in combination with Leniolisib. - Food Interactions
- Take with or without food. Food has negligible effects on systemic exposure of leniolisib.
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 Leniolisib phosphate 3700M1H39Q 1354691-97-6 XXEDEGOAYSGNPS-ZOWNYOTGSA-N - Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Joenja Tablet, film coated 70 mg/1 Oral Pharming Healthcare Inc. 2023-03-29 Not applicable US
Categories
- Drug Categories
- BCRP/ABCG2 Inhibitors
- BCRP/ABCG2 Substrates
- Cytochrome P-450 CYP1A2 Inhibitors
- Cytochrome P-450 CYP1A2 Inhibitors (strength unknown)
- Cytochrome P-450 CYP1A2 Substrates
- Cytochrome P-450 CYP2D6 Substrates
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 CYP3A5 Substrates
- Cytochrome P-450 Enzyme Inhibitors
- Cytochrome P-450 Substrates
- Kinase Inhibitor
- OATP1B1/SLCO1B1 Inhibitors
- OATP1B3 inhibitors
- P-glycoprotein substrates
- Classification
- Not classified
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- L22772Z9CP
- CAS number
- 1354690-24-6
- InChI Key
- MWKYMZXCGYXLPL-ZDUSSCGKSA-N
- InChI
- InChI=1S/C21H25F3N6O2/c1-3-18(31)30-6-4-13(10-30)28-19-15-11-29(7-5-17(15)26-12-27-19)14-8-16(21(22,23)24)20(32-2)25-9-14/h8-9,12-13H,3-7,10-11H2,1-2H3,(H,26,27,28)/t13-/m0/s1
- IUPAC Name
- 1-[(3S)-3-({6-[6-methoxy-5-(trifluoromethyl)pyridin-3-yl]-5H,6H,7H,8H-pyrido[4,3-d]pyrimidin-4-yl}amino)pyrrolidin-1-yl]propan-1-one
- SMILES
- CCC(=O)N1CC[C@@H](C1)NC1=C2CN(CCC2=NC=N1)C1=CN=C(OC)C(=C1)C(F)(F)F
References
- General References
- Michalovich D, Nejentsev S: Activated PI3 Kinase Delta Syndrome: From Genetics to Therapy. Front Immunol. 2018 Feb 27;9:369. doi: 10.3389/fimmu.2018.00369. eCollection 2018. [Article]
- Rao VK, Webster S, Dalm VASH, Sediva A, van Hagen PM, Holland S, Rosenzweig SD, Christ AD, Sloth B, Cabanski M, Joshi AD, de Buck S, Doucet J, Guerini D, Kalis C, Pylvaenaeinen I, Soldermann N, Kashyap A, Uzel G, Lenardo MJ, Patel DD, Lucas CL, Burkhart C: Effective "activated PI3Kdelta syndrome"-targeted therapy with the PI3Kdelta inhibitor leniolisib. Blood. 2017 Nov 23;130(21):2307-2316. doi: 10.1182/blood-2017-08-801191. Epub 2017 Sep 29. [Article]
- Hoegenauer K, Soldermann N, Zecri F, Strang RS, Graveleau N, Wolf RM, Cooke NG, Smith AB, Hollingworth GJ, Blanz J, Gutmann S, Rummel G, Littlewood-Evans A, Burkhart C: Discovery of CDZ173 (Leniolisib), Representing a Structurally Novel Class of PI3K Delta-Selective Inhibitors. ACS Med Chem Lett. 2017 Aug 25;8(9):975-980. doi: 10.1021/acsmedchemlett.7b00293. eCollection 2017 Sep 14. [Article]
- De Buck S, Kucher K, Hara H, Gray C, Woessner R: CYP3A but not P-gp plays a relevant role in the in vivo intestinal and hepatic clearance of the delta-specific phosphoinositide-3 kinase inhibitor leniolisib. Biopharm Drug Dispos. 2018 Sep;39(8):394-402. doi: 10.1002/bdd.2157. [Article]
- Pearson D, Garnier M, Luneau A, James AD, Walles M: (19)F-NMR-based determination of the absorption, metabolism and excretion of the oral phosphatidylinositol-3-kinase (PI3K) delta inhibitor leniolisib (CDZ173) in healthy volunteers. Xenobiotica. 2019 Aug;49(8):953-960. doi: 10.1080/00498254.2018.1523488. Epub 2018 Nov 29. [Article]
- Fresno Vara JA, Casado E, de Castro J, Cejas P, Belda-Iniesta C, Gonzalez-Baron M: PI3K/Akt signalling pathway and cancer. Cancer Treat Rev. 2004 Apr;30(2):193-204. doi: 10.1016/j.ctrv.2003.07.007. [Article]
- Osaki M, Oshimura M, Ito H: PI3K-Akt pathway: its functions and alterations in human cancer. Apoptosis. 2004 Nov;9(6):667-76. doi: 10.1023/B:APPT.0000045801.15585.dd. [Article]
- Martini M, De Santis MC, Braccini L, Gulluni F, Hirsch E: PI3K/AKT signaling pathway and cancer: an updated review. Ann Med. 2014 Sep;46(6):372-83. doi: 10.3109/07853890.2014.912836. Epub 2014 Jun 5. [Article]
- FDA Approved Drug Products: JOENJA (leniolisib) tablets, for oral use [Link]
- FDA News: FDA approves first treatment for activated phosphoinositide 3-kinase delta syndrome [Link]
- External Links
- ChemSpider
- 52083264
- BindingDB
- 118299
- 2633005
- ChEMBL
- CHEMBL3643413
- PDBe Ligand
- 9NQ
- Wikipedia
- Leniolisib
- PDB Entries
- 5o83
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 3 Recruiting Treatment APDS 2 3 Recruiting Treatment APDS Gene Mutation 1 2 Completed Treatment Primary Sjögren's Syndrome (pSS) 1 2, 3 Active Not Recruiting Treatment Activated PI3Kdelta Syndrome (APDS); PASLI Disease 1 2, 3 Completed Treatment Common Variable Immunodeficiency (CVID), APDS / PASLI 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Tablet, film coated Oral 70 mg/1 - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US8653092 No 2014-02-18 2032-02-19 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source water solubility <1 mg/mL https://www.selleckchem.com/msds/MSDS_S8752.pdf - Predicted Properties
Property Value Source logP 2.01 Chemaxon pKa (Strongest Acidic) 18.21 Chemaxon pKa (Strongest Basic) 5.43 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 7 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 83.48 Å2 Chemaxon Rotatable Bond Count 6 Chemaxon Refractivity 115.08 m3·mol-1 Chemaxon Polarizability 43.46 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, Negative (Annotated) Predicted LC-MS/MS splash10-006t-0000900000-a2bcc1cab0dd31e6e136 Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS splash10-0udi-0004900000-37e9b0f773ad7325777e Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-0udj-0007900000-0912d4197d70801ce729 Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-03di-0019200000-31c01db42cf066b2187a Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-004j-0009100000-788f8eaee2206e82ebac Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-014l-1239200000-5a63f6ccab314f41063a 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
![](https://go.drugbank.com/assets/locked/DrugTargets2-682eb846d210ae4bf33ca03febccfb57bb1c61318e699b729e5df4dfab2c5b67.png)
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Phosphatidylinositol-4,5-bisphosphate 3-kinase activity
- Specific Function
- Phosphoinositide-3-kinase (PI3K) that phosphorylates PftdIns(4,5)P2 (Phosphatidylinositol 4,5-bisphosphate) to generate phosphatidylinositol 3,4,5-trisphosphate (PIP3). PIP3 plays a key role by rec...
- Gene Name
- PIK3CD
- Uniprot ID
- O00329
- Uniprot Name
- Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform
- Molecular Weight
- 119478.065 Da
References
- Rao VK, Webster S, Dalm VASH, Sediva A, van Hagen PM, Holland S, Rosenzweig SD, Christ AD, Sloth B, Cabanski M, Joshi AD, de Buck S, Doucet J, Guerini D, Kalis C, Pylvaenaeinen I, Soldermann N, Kashyap A, Uzel G, Lenardo MJ, Patel DD, Lucas CL, Burkhart C: Effective "activated PI3Kdelta syndrome"-targeted therapy with the PI3Kdelta inhibitor leniolisib. Blood. 2017 Nov 23;130(21):2307-2316. doi: 10.1182/blood-2017-08-801191. Epub 2017 Sep 29. [Article]
- Hoegenauer K, Soldermann N, Zecri F, Strang RS, Graveleau N, Wolf RM, Cooke NG, Smith AB, Hollingworth GJ, Blanz J, Gutmann S, Rummel G, Littlewood-Evans A, Burkhart C: Discovery of CDZ173 (Leniolisib), Representing a Structurally Novel Class of PI3K Delta-Selective Inhibitors. ACS Med Chem Lett. 2017 Aug 25;8(9):975-980. doi: 10.1021/acsmedchemlett.7b00293. eCollection 2017 Sep 14. [Article]
- FDA Approved Drug Products: JOENJA (leniolisib) tablets, for oral use [Link]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- SubstrateInhibitor
- Curator comments
- Leniolisib inhibits CYP1A2 in a time-dependent manner in vitro.
- 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
- FDA Approved Drug Products: JOENJA (leniolisib) tablets, for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- 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
- De Buck S, Kucher K, Hara H, Gray C, Woessner R: CYP3A but not P-gp plays a relevant role in the in vivo intestinal and hepatic clearance of the delta-specific phosphoinositide-3 kinase inhibitor leniolisib. Biopharm Drug Dispos. 2018 Sep;39(8):394-402. doi: 10.1002/bdd.2157. [Article]
- FDA Approved Drug Products: JOENJA (leniolisib) tablets, for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Oxygen binding
- 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
- CYP3A5
- Uniprot ID
- P20815
- Uniprot Name
- Cytochrome P450 3A5
- Molecular Weight
- 57108.065 Da
References
- FDA Approved Drug Products: JOENJA (leniolisib) tablets, for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- 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
- FDA Approved Drug Products: JOENJA (leniolisib) tablets, for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Vitamin d 24-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
- CYP1A1
- Uniprot ID
- P04798
- Uniprot Name
- Cytochrome P450 1A1
- Molecular Weight
- 58164.815 Da
References
- De Buck S, Kucher K, Hara H, Gray C, Woessner R: CYP3A but not P-gp plays a relevant role in the in vivo intestinal and hepatic clearance of the delta-specific phosphoinositide-3 kinase inhibitor leniolisib. Biopharm Drug Dispos. 2018 Sep;39(8):394-402. doi: 10.1002/bdd.2157. [Article]
- FDA Approved Drug Products: JOENJA (leniolisib) tablets, for oral use [Link]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- SubstrateInhibitor
- Curator comments
- In vitro, leniolisib is a substrate and an inhibitor of the hepatic efflux transporter BCRP.
- 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
- FDA Approved Drug Products: JOENJA (leniolisib) tablets, for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- Curator comments
- Leniolisib was identified as a potential inhibitor of this transporter 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
- FDA Approved Drug Products: JOENJA (leniolisib) tablets, for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- Curator comments
- Leniolisib was identified as a potential inhibitor of this transporter 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
- FDA Approved Drug Products: JOENJA (leniolisib) tablets, for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- Curator comments
- Leniolisib was a substrate of P-glycoprotein 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
- FDA Approved Drug Products: JOENJA (leniolisib) tablets, for oral use [Link]
Drug created at December 15, 2020 18:15 / Updated at April 11, 2023 23:56