Identification
- Summary
Acalabrutinib is a Bruton tyrosine kinase inhibitor used to treat mantle cell lymphoma, chronic lymphocytic leukemia, and small lymphocytic lymphoma.
- Brand Names
- Calquence
- Generic Name
- Acalabrutinib
- DrugBank Accession Number
- DB11703
- Background
To date, acalabrutinib has been used in trials studying the treatment of B-All, myelofibrosis, ovarian cancer, multiple myeloma, and Hodgkin lymphoma, among others.
As of October 31, 2017 the FDA approved Astra Zeneca's orally administered Calquence (acalabrutinib, capsules). This Bruton tyrosine kinase (BTK) inhibitor indicated for the treatment of chronic lymphocytic leukemia, small lymphocytic lymphoma, and in adult patients with Mantle cell lymphoma (MCL) who have already received at least one prior therapy.6 In August 2022, the FDA approved a new tablet formulation of Calquence, enabling the co-administration of this drug with proton pump inhibitors (PPIs).7,8 Unlike Calquence capsules, the co-administration of Calquence tablets and PPIs does not have an effect in the pharmacokinetics of acalabrutinib.6,7
Also known as ACP-196, acalabrutinib is also considered a second generation BTK inhibitor because it was rationally designed to be more potent and selective than ibrutinib, theoretically expected to demonstrate fewer adverse effects owing to minimized bystander effects on targets other than BTK.
Nevertheless, acalabrutinib was approved under the FDA's accelerated approval pathway, which is based upon overall response rate and faciliates earlier approval of medicines that treat serious conditions or/and that fill an unmet medical need based on a surrogate endpoint. Continued approval for acalabrutinib's currently accepted indication may subsequently be contingent upon ongoing verification and description of clinical benefit in confimatory trials.
Furthermore, the FDA granted this medication Priority Review and Breakthrough Therapy designations. It also received Orphan Drug designation, which provides incentives to assist and encourage the development of drugs for rare diseases. At this time, more than 35 clinical trials across 40 countries with more than 2500 patients are underway or have been completed with regards to further research into better understanding and expanding the therapeutic uses of acalabrutinib 5.
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
Structure for Acalabrutinib (DB11703)
- Weight
- Average: 465.517
Monoisotopic: 465.191323009 - Chemical Formula
- C26H23N7O2
- Synonyms
- Acalabrutinib
- Acalabrutinibum
- External IDs
- ACP-196
Pharmacology
- Indication
Acalabrutinib is currently indicated for the treatment of adult patients with Mantle Cell Lymphoma (MCL) who have received at least one prior therapy.6 It has also been recently approved for chronic lymphocytic leukemia and small lymphocytic lymphoma.6
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 Treatment of Chronic lymphocytic leukaemia (cll) •••••••••••• Treatment of Mantle cell lymphoma •••••••••••• ••••• • • ••••• ••••••• ••• •••••• •••• •••••••• Treatment of Small lymphocytic lymphoma (sll) •••••••••••• - Contraindications & Blackbox Warnings
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Acalabrutinib is a Bruton Tyrosine Kinase inhibitor that prevents the proliferation, trafficking, chemotaxis, and adhesion of B cells.6 It is taken every 12 hours and can cause other effects such as atrial fibrillation, other malignancies, cytopenia, hemorrhage, and infection.6
- Mechanism of action
Mantle Cell Lymphoma (MCL) is a rare yet aggressive type of B-cell non-Hodgkin lymphoma (NHL) with poor prognosis 2,4. Subsequently, relapse is common in MCL patients and ultimately represents disease progression 4.
Lymphoma occurs when immune system lymphocytes grow and multiply uncontrollably. Such cancerous lymphocytes may travel to many parts of the body, including the lymph nodes, spleen, bone marrow, blood, and other organs where they can multiply and form a mass(es) called a tumor. One of the main kinds of lymphocytes that can develop into cancerous lymphomas are the body's own B-lymphocytes (B-cells) 4.
Bruton Tyrosine Kinase (BTK) is a signalling molecule of the B-cell antigen receptor and cytokine receptor pathways. Such BTK signaling causes the activation of pathways necessary for B-cell proliferation, trafficking, chemotaxis, and adhesion.6
Acalabrutinib is a small molecule inhibitor of BTK. Both acalabrutinib and its active metabolite, ACP-5862, act to form a covalent bond with a cysteine residue (Cys481) in the BTK active site, leading to inhibition of BTK enzymatic activity.2,4 As a result, acalabrutinib inhibits BTK-mediated activation of downstream signaling proteins CD86 and CD69, which ultimately inhibits malignant B-cell proliferation and survival4
Whereas ibrutinib is typically recognized as the first-in-class BTK inhibitor,2 acalabrutinib is considered a second generation BTK inhibitor primarily because it demonstrates highter selectivity and inhibition of the targeted activity of BTK while having a much greater IC50 or otherwise virtually no inhibition on the kinase activities of ITK, EGFR, ERBB2, ERBB4, JAK3, BLK, FGR, FYN, HCK, LCK, LYN, SRC, and YES1.2
In effect, acalabrutinib was rationally designed to be more potent and selective than ibrutinib, all the while demonstrating fewer adverse effects - in theory - because of the drug's minimized off target effects.
Target Actions Organism ATyrosine-protein kinase BTK inhibitorHumans - Absorption
The geometric mean absolute bioavailability of acalabrutinib is 25% with a median time to peak plasma concentrations (Tmax) of 0.75 hours.6
- Volume of distribution
The mean steady-state volume of distribution is approximately 34 L.6
- Protein binding
Reversible binding of acalabrutinib to human plasma protein is approximately 97.5%. The in vitro mean blood-to-plasma ratio is about 0.7.6 In vitro experiments at physiologic concentrations show that acalabrutinib can be 93.7% bound to human serum albumin and 41.1% bound to alpha-1-acid glycoprotein.3
- Metabolism
Acalabrutinib is mainly metabolized by CYP3A enzymes. ACP-5862 is identified to be the major active metabolite in plasma with a geometric mean exposure (AUC) that is about 2-3 times greater than the exposure of acalabrutinib. ACP-5862 is about 50% less potent than acalabrutinib in regards to the inhibition of BTK.6
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- Route of elimination
After administration of a single 100 mg radiolabelled acalabrutinib dose in healthy subjects, 84% of the dose was recovered in the feces and 12% of the dose was recovered in the urine.6 An irradiated dose of acalabrutinib was 34.7% recovered as the metabolite ACP-5862; 8.6% was recovered as unchanged acalabrutinub; 10.8 was recovered as a mixture of the M7, M8, M9, M10, and M11 metabolites; 5.9% was the M25 metabolite; 2.5% was recovered as the M3 metabolite.3
- Half-life
After administering a single oral dose of 100 mg acalabrutinib, the median terminal elimination half-life of the drug was found to be 0.9 (with a range of 0.6 to 2.8) hours.6
The half-life of the active metabolite, ACP-5862, is about 6.9 hours.6
- Clearance
Acalabrutinib's mean apparent oral clearance (CL/F) is observed to be 159 L/hr with similar PK between patients and healthy subjects, based on population PK analysis.6
- Adverse Effects
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Data regarding the toxicity of acalabrutinib is not readily available.6
- 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 softwareAbametapir The serum concentration of Acalabrutinib can be increased when it is combined with Abametapir. Abatacept The metabolism of Acalabrutinib can be increased when combined with Abatacept. Abemaciclib The metabolism of Abemaciclib can be decreased when combined with Acalabrutinib. Acenocoumarol The serum concentration of Acenocoumarol can be increased when it is combined with Acalabrutinib. Acetaminophen The metabolism of Acalabrutinib can be increased when combined with Acetaminophen. - Food Interactions
- Avoid grapefruit products. Grapefruit inhibits CYP3A metabolism, which may increase the serum concentration of acalabrutinib. Dose adjustment may be necessary if co-administered.
- Exercise caution with St. John's Wort. The official product labeling recommends avoiding strong CYP3A4 inducers. This herb induces CYP3A metabolism and may reduce serum levels of acalabrutinib.
- Take separate from antacids. Take at least 2 hours before or after antacids.
- Take with a full glass of water.
- 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.- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Calquence Capsule 100 mg Oral Astra Zeneca Ab 2020-12-16 Not applicable EU 
Calquence Capsule 100 mg Oral Astra Zeneca 2019-10-02 Not applicable Canada 
Calquence Tablet, film coated 100 mg Oral Astra Zeneca Ab 2023-04-04 Not applicable EU Calquence Capsule 100 mg Oral Astra Zeneca Ab 2020-12-16 Not applicable EU Calquence Capsule, gelatin coated 100 mg/1 Oral AstraZeneca Pharmaceuticals LP 2017-10-31 Not applicable US 
Categories
- ATC Codes
- L01EL02 — Acalabrutinib
- Drug Categories
- Acids, Carbocyclic
- Amides
- Antineoplastic Agents
- Antineoplastic and Immunomodulating Agents
- Benzene Derivatives
- Benzoates
- Bruton's tyrosine kinase (BTK) inhibitors
- Cytochrome P-450 CYP3A Inhibitors
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Inhibitors
- Cytochrome P-450 CYP3A4 Inhibitors (weak)
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 CYP3A4 Substrates with a Narrow Therapeutic Index
- Cytochrome P-450 CYP3A5 Inhibitors
- Cytochrome P-450 CYP3A5 Inhibitors (weak)
- Cytochrome P-450 Enzyme Inhibitors
- Cytochrome P-450 Substrates
- Enzyme Inhibitors
- Kinase Inhibitor
- Narrow Therapeutic Index Drugs
- Protein Kinase Inhibitors
- Tyrosine Kinase Inhibitors
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as phenylimidazoles. These are polycyclic aromatic compounds containing a benzene ring linked to an imidazole ring through a CC or CN bond.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Azoles
- Sub Class
- Imidazoles
- Direct Parent
- Phenylimidazoles
- Alternative Parents
- Benzamides / Imidazo[1,5-a]pyrazines / Benzoyl derivatives / N-acylpyrrolidines / Aminopyrazines / N-substituted imidazoles / Imidolactams / Pyridines and derivatives / Heteroaromatic compounds / Tertiary carboxylic acid amides show 7 more
- Substituents
- 4-phenylimidazole / 5-phenylimidazole / Amine / Amino acid or derivatives / Aminopyrazine / Aromatic heteropolycyclic compound / Azacycle / Benzamide / Benzenoid / Benzoic acid or derivatives show 22 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- Not Available
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- I42748ELQW
- CAS number
- 1420477-60-6
- InChI Key
- WDENQIQQYWYTPO-IBGZPJMESA-N
- InChI
- InChI=1S/C26H23N7O2/c1-2-6-21(34)32-15-5-7-19(32)25-31-22(23-24(27)29-14-16-33(23)25)17-9-11-18(12-10-17)26(35)30-20-8-3-4-13-28-20/h3-4,8-14,16,19H,5,7,15H2,1H3,(H2,27,29)(H,28,30,35)/t19-/m0/s1
- IUPAC Name
- 4-{8-amino-3-[(2S)-1-(but-2-ynoyl)pyrrolidin-2-yl]imidazo[1,5-a]pyrazin-1-yl}-N-(pyridin-2-yl)benzamide
- SMILES
- CC#CC(=O)N1CCC[C@H]1C1=NC(=C2N1C=CN=C2N)C1=CC=C(C=C1)C(=O)NC1=CC=CC=N1
References
- General References
- Wu J, Zhang M, Liu D: Acalabrutinib (ACP-196): a selective second-generation BTK inhibitor. J Hematol Oncol. 2016 Mar 9;9:21. doi: 10.1186/s13045-016-0250-9. [Article]
- Cheah CY, Seymour JF, Wang ML: Mantle Cell Lymphoma. J Clin Oncol. 2016 Apr 10;34(11):1256-69. doi: 10.1200/JCO.2015.63.5904. Epub 2016 Jan 11. [Article]
- Podoll T, Pearson PG, Evarts J, Ingallinera T, Bibikova E, Sun H, Gohdes M, Cardinal K, Sanghvi M, Slatter JG: Bioavailability, Biotransformation, and Excretion of the Covalent Bruton Tyrosine Kinase Inhibitor Acalabrutinib in Rats, Dogs, and Humans. Drug Metab Dispos. 2019 Feb;47(2):145-154. doi: 10.1124/dmd.118.084459. Epub 2018 Nov 15. [Article]
- Lymphoma Research Foundation's Getting the Facts: Mantle Cell Lymphoma - Relapsed/Refractory [Link]
- Astra Zeneca Press Release: US FDA Approves Astrazeneca's Calquence for Adult Patients with Previously-Treated Mantle Cell Lymphoma [Link]
- FDA Approved Drug Products: Calquence Acalabrutinib Oral Capsules [Link]
- FDA Approved Drug Products: Calquence (acalabrutinib) tablets for oral use [Link]
- Bloomberg: CALQUENCE (acalabrutinib) tablet formulation approved in the US across current indications [Link]
- External Links
- PubChem Compound
- 71226662
- PubChem Substance
- 347828068
- ChemSpider
- 36764951
- BindingDB
- 50175583
- 1986808
- ChEBI
- 167707
- ChEMBL
- CHEMBL3707348
- ZINC
- ZINC000208774715
- PDBe Ligand
- XQQ
- Wikipedia
- Acalabrutinib
- PDB Entries
- 8fd9
- FDA label
- Download (492 KB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Completed Treatment Chronic Lymphocytic Leukemia and Relapsed and Refractory Mantle Cell Lymphoma 1 3 Active Not Recruiting Treatment Chronic Lymphocytic Leukemia 4 3 Active Not Recruiting Treatment Chronic Lymphocytic Leukemia- Binet Staging System 1 3 Active Not Recruiting Treatment Mantle Cell Lymphoma (MCL) 1 3 Active Not Recruiting Treatment Untreated Chronic Lymphocytic Leukemia 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Capsule Oral 100 mg Capsule, gelatin coated Oral 100 mg/1 Tablet, film coated Oral 100 mg Tablet, film coated Oral 100 mg/1 Capsule, coated Oral 100 mg - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US9796721 No 2017-10-24 2036-07-01 US US9758524 No 2017-09-12 2032-07-11 US US9290504 No 2016-03-22 2032-07-11 US US7459554 No 2008-12-02 2026-11-24 US US10167291 No 2019-01-01 2036-07-01 US US10272083 No 2019-04-30 2035-01-21 US US10239883 No 2019-03-26 2032-07-11 US US11059829 No 2021-07-13 2036-07-01 US US11771696 No 2015-01-21 2035-01-21 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source water solubility Freely soluble in water at pH values below 3 but is practically insoluble in water at pH values above 6 FDA Label logP 0.49 ChemSpider - Predicted Properties
Property Value Source Water Solubility 0.0109 mg/mL ALOGPS logP 2.69 ALOGPS logP 2.56 Chemaxon logS -4.6 ALOGPS pKa (Strongest Acidic) 12.34 Chemaxon pKa (Strongest Basic) 5 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 6 Chemaxon Hydrogen Donor Count 2 Chemaxon Polar Surface Area 118.51 Å2 Chemaxon Rotatable Bond Count 5 Chemaxon Refractivity 135.72 m3·mol-1 Chemaxon Polarizability 51 Å3 Chemaxon Number of Rings 5 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter No 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 splash10-00di-0009100000-1a9cd814020eb48227c0 Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-03k9-0001900000-ab75d44782140dab6c84 Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-05fr-0009100000-9dcaefad44b121c78046 Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-01p6-3002900000-3712512f3b94661751f5 Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-001a-2059200000-f26af6f03d638dad5032 Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-0f96-7039400000-6d5b629265d744b5e69e 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]- 195.473 predictedDeepCCS 1.0 (2019) [M+H]+ 197.86858 predictedDeepCCS 1.0 (2019) [M+Na]+ 203.7811 predictedDeepCCS 1.0 (2019)
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Protein tyrosine kinase activity
- Specific Function
- Non-receptor tyrosine kinase indispensable for B lymphocyte development, differentiation and signaling. Binding of antigen to the B-cell antigen receptor (BCR) triggers signaling that ultimately le...
- Gene Name
- BTK
- Uniprot ID
- Q06187
- Uniprot Name
- Tyrosine-protein kinase BTK
- Molecular Weight
- 76280.71 Da
References
- Bond DA, Woyach JA: Targeting BTK in CLL: Beyond Ibrutinib. Curr Hematol Malig Rep. 2019 Jun;14(3):197-205. doi: 10.1007/s11899-019-00512-0. [Article]
- Wilkinson T, Dixon R, Page C, Carroll M, Griffiths G, Ho LP, De Soyza A, Felton T, Lewis KE, Phekoo K, Chalmers JD, Gordon A, McGarvey L, Doherty J, Read RC, Shankar-Hari M, Martinez-Alier N, O'Kelly M, Duncan G, Walles R, Sykes J, Summers C, Singh D: ACCORD: A Multicentre, Seamless, Phase 2 Adaptive Randomisation Platform Study to Assess the Efficacy and Safety of Multiple Candidate Agents for the Treatment of COVID-19 in Hospitalised Patients: A structured summary of a study protocol for a randomised controlled trial. Trials. 2020 Jul 31;21(1):691. doi: 10.1186/s13063-020-04584-9. [Article]
- Castillo JJ, Treon SP: What is new in the treatment of Waldenstrom macroglobulinemia? Leukemia. 2019 Nov;33(11):2555-2562. doi: 10.1038/s41375-019-0592-8. Epub 2019 Oct 7. [Article]
- Zheng TJ, Lofurno ER, Melrose AR, Lakshmanan HHS, Pang J, Phillips KG, Fallon ME, Kohs TCL, Ngo ATP, Shatzel JJ, Hinds MT, McCarty OJT, Aslan JE: Assessment of the effects of Syk and BTK inhibitors on GPVI-mediated platelet signaling and function. Am J Physiol Cell Physiol. 2021 May 1;320(5):C902-C915. doi: 10.1152/ajpcell.00296.2020. Epub 2021 Mar 10. [Article]
- Kaliamurthi S, Selvaraj G, Selvaraj C, Singh SK, Wei DQ, Peslherbe GH: Structure-Based Virtual Screening Reveals Ibrutinib and Zanubrutinib as Potential Repurposed Drugs against COVID-19. Int J Mol Sci. 2021 Jun 30;22(13). pii: ijms22137071. doi: 10.3390/ijms22137071. [Article]
- FDA Approved Drug Products: Calquence Acalabrutinib Oral Capsules [Link]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- 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: Calquence Acalabrutinib Oral Capsules [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- 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: Calquence Acalabrutinib Oral Capsules [Link]
- Kind
- Protein group
- 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...
Components:
| Name | UniProt ID |
|---|---|
| Cytochrome P450 3A4 | P08684 |
| Cytochrome P450 3A43 | Q9HB55 |
| Cytochrome P450 3A5 | P20815 |
| Cytochrome P450 3A7 | P24462 |
References
- FDA Approved Drug Products: Calquence Acalabrutinib Oral Capsules [Link]
Carriers
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- 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
- Abdelhameed AS, Alanazi AM, Bakheit AH, Hassan ES, Herqash RN, Almutairi FM: Novel BTK inhibitor acalabrutinib (ACP-196) tightly binds to site I of the human serum albumin as observed by spectroscopic and computational studies. Int J Biol Macromol. 2019 Apr 15;127:536-543. doi: 10.1016/j.ijbiomac.2019.01.083. Epub 2019 Jan 18. [Article]
- Podoll T, Pearson PG, Evarts J, Ingallinera T, Bibikova E, Sun H, Gohdes M, Cardinal K, Sanghvi M, Slatter JG: Bioavailability, Biotransformation, and Excretion of the Covalent Bruton Tyrosine Kinase Inhibitor Acalabrutinib in Rats, Dogs, and Humans. Drug Metab Dispos. 2019 Feb;47(2):145-154. doi: 10.1124/dmd.118.084459. Epub 2018 Nov 15. [Article]
- Kind
- Protein group
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Binder
- General Function
- Not Available
- Specific Function
- Functions as transport protein in the blood stream. Binds various ligands in the interior of its beta-barrel domain. Also binds synthetic drugs and influences their distribution and availability in...
Components:
References
- Podoll T, Pearson PG, Evarts J, Ingallinera T, Bibikova E, Sun H, Gohdes M, Cardinal K, Sanghvi M, Slatter JG: Bioavailability, Biotransformation, and Excretion of the Covalent Bruton Tyrosine Kinase Inhibitor Acalabrutinib in Rats, Dogs, and Humans. Drug Metab Dispos. 2019 Feb;47(2):145-154. doi: 10.1124/dmd.118.084459. Epub 2018 Nov 15. [Article]
Drug created at October 20, 2016 20:41 / Updated at February 20, 2024 23:54