Copanlisib

Identification

Summary

Copanlisib is a PI3K inhibitor used to treat relapsed follicular lymphoma in adults.

Brand Names
Aliqopa
Generic Name
Copanlisib
DrugBank Accession Number
DB12483
Background

Copanlisib is a selective pan-Class I phosphoinositide 3-kinase (PI3K) inhibitor with preferential activity against the alpha and delta isoforms. PI3K, a lipid kinase that activates downstream signalling pathways involved in cell survival and growth, that exists in different isoforms and is often overexpressed in hematological malignancies.2 Copanlisib was granted accelerated approval by the FDA in September 2017 for the treatment of follicular lymphoma.1

Type
Small Molecule
Groups
Approved, Investigational
Structure
Weight
Average: 480.529
Monoisotopic: 480.223351414
Chemical Formula
C23H28N8O4
Synonyms
  • 2-AMINO-N-(7-METHOXY-8-(3-(MORPHOLIN-4-YL)PROPOXY)-2,3-DIHYDROIMIDAZO(1,2-C)QUINAZOLIN-5-YL(PYRIMIDINE-5-CARBOXAMIDE
  • 2-AMINO-N-(7-METHOXY-8-(3-MORPHOLIN-4-YLPROPOXY)-2,3-DIHYDROIMIDAZO(1,2-C)QUINAZOLIN-5-YL)PYRIMIDINE-5-CARBOXAMIDE
  • 5-PYRIMIDINECARBOXAMIDE, 2-AMINO-N-(2,3-DIHYDRO-7-METHOXY-8-(3-(4-MORPHOLINYL)PROPOXY)IMIDAZO(1,2-C)QUINAZOLIN-5-YL)-
  • Copanlisib
External IDs
  • BAY 80-6946
  • BAY-80-6946
  • BAY80-6946

Pharmacology

Indication

Copanlisib is indicated for the treatment of adults with relapsed follicular lymphoma (FL) who have received at least two prior systemic therapies. This indication was granted under accelerated approval; thus, continued approval may be contingent upon verification and description of clinical benefit in a confirmatory trial.5

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Treatment ofRelapsed follicular lymphoma••••••••••••••••••• ••••• ••• ••••• •••••••• •••••••••
Contraindications & Blackbox Warnings
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Pharmacodynamics

Copanlisib is a kinase inhibitor with anti-tumour and pro-apoptotic activity in various tumour cell lines and xenograft models. Copanlisib causes an elevation in plasma glucose levels.5

Mechanism of action

Phosphatidylinositol-3-kinase (PI3K) signalling pathway is implicated in cell proliferation and survival, as well as resistance to chemotherapeutic agents. PI3K isoforms are often overexpressed in B-cell malignancies, including follicular lymphoma.2 Copanlisib is a class I PI3K inhibitor with preferential activity against PI3K-α and PI3K-δ isoforms expressed in malignant B cells. It binds with IC50 values of 0.5, 3.7, 6.4, and 0.7 nmol/L against class I PI3K-α, β, γ, and δ isoforms, respectively.1 Copanlisibinduces tumour cell death by apoptosis, blocks cell cycle progression, and inhibits the proliferation of primary malignant B cell lines. Copanlisib inhibits several key cell signalling pathways, including B-cell receptor (BCR) signalling, CXCR12-mediated chemotaxis of malignant B cells, and NFκB signalling in lymphoma cell lines.1,5

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

The area under the plasma concentration-time curve (AUC) and maximum plasma concentration (Cmax) of copanlisib increase dose-proportionally over 5 to 93 mg (0.08 to 1.55 times the approved recommended dose) absolute dose range and exhibit linear pharmacokinetics (PK). There is no time-dependency and no accumulation in the pharmacokinetics of copanlisib. The geometric mean (range) steady state copanlisib exposure at 0.8 mg/kg (approximately the approved recommended dose of 60 mg) are 463 (range: 105 to 1670; SD: 584) ng/mL for Cmax and 1570 (range: 536 to 3410; SD: 338) ng x hr/mL for AUC0-25h.5

Volume of distribution

The geometric mean volume of distribution is 871 (range: 423 to 2150; SD: 479) L.5

Protein binding

Copanlisib is 84.2% bound to plasma proteins, mainly to serum albumin. The in vitro mean blood-to-plasma ratio is 1.7, with a range from 1.5 to 2.1.5

Metabolism

Copanlisib is primarily metabolized by CYP3A (>90%) and to a lesser extent, CYP1A1 (<10%).3,5 The M1 metabolite accounts for 5% of total radioactivity in plasma and has a pharmacological activity that is comparable to that of the parent compound.3,5

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Route of elimination

In humans, approximately half of copanlisib is excreted as unchanged parent compound and the other half is excreted as metabolites. Following a single intravenous dose of 12 mg (0.2 times the recommended approved dose) radiolabeled copanlisib, approximately 64% of the administered dose was recovered in feces and 22% in urine within 20 to 34 days. Unchanged copanlisib represented approximately 30% of the administered dose in feces and 15% in urine. Metabolites resulting from CYP450-mediated oxidation accounted for 41% of the administered dose.5

Half-life

The geometric mean terminal elimination half-life of copanlisib is 39.1 (range: 14.6 to 82.4; SD: 15.0) hours.5

Clearance

The geometric mean clearance is 17.9 (range: 7.3 to 51.4; SD: 8.5) L/hr.5

Adverse Effects
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Toxicity

The LD50 of copanlisib dihydrochloride in male and female rats after a single intravenous dose administration was >23.0 mg/kg, which corresponds to 20.0 mg/kg copanlisib.6 There is no information on copanlisib overdose.

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 Copanlisib can be increased when it is combined with Abametapir.
AbataceptThe metabolism of Copanlisib can be increased when combined with Abatacept.
AbemaciclibAbemaciclib may decrease the excretion rate of Copanlisib which could result in a higher serum level.
AcalabrutinibThe metabolism of Copanlisib can be decreased when combined with Acalabrutinib.
AcetaminophenThe metabolism of Copanlisib can be increased when combined with Acetaminophen.
Food Interactions
  • Avoid grapefruit products. Grapefruit strongly inhibits CYP3A metabolism, which may increase the serum concentration of copanlisib.
  • Avoid St. John's Wort. This herb strongly induces the CYP3A metabolism of copanlisib and may reduce its serum concentration.

Products

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Product Ingredients
IngredientUNIICASInChI Key
Copanlisib dihydrochloride03ZI7RZ52O1402152-13-9STGQPVQAAFJJFX-UHFFFAOYSA-N
Copanlisib dihydrochloride hydrateW421JK3CPA1402152-46-8PRZNRMHJLYLVBJ-UHFFFAOYSA-N
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
AliqopaInjection, powder, lyophilized, for solution15 mg/1mLIntravenousBayer HealthCare Pharmaceuticals Inc.2017-09-14Not applicableUS flag

Categories

ATC Codes
L01EM02 — Copanlisib
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as quinazolinamines. These are heterocyclic aromatic compounds containing a quianazoline moiety substituted by one or more amine groups.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Diazanaphthalenes
Sub Class
Benzodiazines
Direct Parent
Quinazolinamines
Alternative Parents
Pyrimidinecarboxamides / Anisoles / Alkyl aryl ethers / Aminopyrimidines and derivatives / Morpholines / Imidolactams / Imidazolines / Heteroaromatic compounds / Trialkylamines / Amino acids and derivatives
show 10 more
Substituents
2-imidazoline / Alkyl aryl ether / Amidine / Amine / Amino acid or derivatives / Aminopyrimidine / Anisole / Aromatic heteropolycyclic compound / Azacycle / Benzenoid
show 27 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
Not Available
Affected organisms
Not Available

Chemical Identifiers

UNII
WI6V529FZ9
CAS number
1032568-63-0
InChI Key
PZBCKZWLPGJMAO-UHFFFAOYSA-N
InChI
InChI=1S/C23H28N8O4/c1-33-19-17(35-10-2-6-30-8-11-34-12-9-30)4-3-16-18(19)28-23(31-7-5-25-20(16)31)29-21(32)15-13-26-22(24)27-14-15/h3-4,13-14H,2,5-12H2,1H3,(H2,24,26,27)(H,28,29,32)
IUPAC Name
2-amino-N-{7-methoxy-8-[3-(morpholin-4-yl)propoxy]-2H,3H-imidazo[1,2-c]quinazolin-5-yl}pyrimidine-5-carboxamide
SMILES
COC1=C(OCCCN2CCOCC2)C=CC2=C1N=C(NC(=O)C1=CN=C(N)N=C1)N1CCN=C21

References

General References
  1. Markham A: Copanlisib: First Global Approval. Drugs. 2017 Dec;77(18):2057-2062. doi: 10.1007/s40265-017-0838-6. [Article]
  2. Mensah FA, Blaize JP, Bryan LJ: Spotlight on copanlisib and its potential in the treatment of relapsed/refractory follicular lymphoma: evidence to date. Onco Targets Ther. 2018 Aug 13;11:4817-4827. doi: 10.2147/OTT.S142264. eCollection 2018. [Article]
  3. Gerisch M, Schwarz T, Lang D, Rohde G, Reif S, Genvresse I, Reschke S, van der Mey D, Granvil C: Pharmacokinetics of intravenous pan-class I phosphatidylinositol 3-kinase (PI3K) inhibitor [(14)C]copanlisib (BAY 80-6946) in a mass balance study in healthy male volunteers. Cancer Chemother Pharmacol. 2017 Sep;80(3):535-544. doi: 10.1007/s00280-017-3383-9. Epub 2017 Jul 11. [Article]
  4. FDA Press Announcements: FDA approves new treatment for adults with relapsed follicular lymphoma [Link]
  5. FDA Approved Drug Products: ALIQOPA (copanlisib) for injection, for intravenous use (September 2023) [Link]
  6. EMA: Aliqopa (copanlisib) withdrawal assessment report [Link]
PubChem Compound
24989044
PubChem Substance
347828721
ChemSpider
25069683
BindingDB
50204093
RxNav
1945077
ChEBI
173077
ChEMBL
CHEMBL3218576
ZINC
ZINC000068247389
PDBe Ligand
6E2
Wikipedia
Copanlisib
PDB Entries
5g2n

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
3Active Not RecruitingTreatmentNon-Hodgkin's Lymphoma (NHL)1
3CompletedTreatmentNon-Hodgkin's Lymphoma (NHL)1
3TerminatedTreatmentNon-Hodgkin's Lymphoma (NHL)1
2Active Not RecruitingScreeningAdvanced Malignant Solid Tumor / Bladder Carcinoma / Breast Carcinoma / Carcinoma of the Head and Neck / Carcinoma of the Skin / Cervical Carcinoma / Colon Carcinoma / Colorectal Carcinoma (CRC) / Endometrial Carcinoma / Esophageal Carcinoma / Gastric Carcinoma / Glioma / Liver and Intrahepatic Bile Duct Carcinoma / Lung Carcinoma / Lymphoma / Malignant Uterine Neoplasm / Melanoma / Multiple Myeloma (MM) / Ovarian Carcinoma / Pancreatic Carcinoma / Prostate Carcinoma / Rectal Carcinoma / Recurrent Bladder Carcinoma / Recurrent Breast Carcinoma / Recurrent Cervical Carcinoma / Recurrent Colon Carcinoma / Recurrent Colorectal Carcinoma / Recurrent Esophageal Carcinoma / Recurrent Gastric Carcinoma / Recurrent Gliomas / Recurrent Head and Neck Carcinoma / Recurrent Liver Carcinoma / Recurrent Lung Carcinoma / Recurrent Lymphoma / Recurrent Malignant Solid Neoplasm / Recurrent Melanoma / Recurrent multiple myeloma / Recurrent Ovarian Carcinoma / Recurrent Pancreatic Carcinoma / Recurrent Prostate Carcinoma / Recurrent Rectal Carcinoma / Recurrent Skin Carcinoma / Recurrent Thyroid Gland Carcinoma / Recurrent Uterine Corpus Cancer / Refractory Lymphomas / Refractory Malignant Solid Neoplasm / Refractory Multiple Myeloma / Renal Carcinoma / Thyroid Gland Carcinoma / Uterine Corpus Cancer1
2Active Not RecruitingTreatmentAdvanced Lymphomas / Advanced Malignant Solid Tumor / Hematopoietic and Lymphoid System Neoplasm / Refractory Lymphomas / Refractory Malignant Solid Neoplasm / Refractory Multiple Myeloma1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Injection, powder, lyophilized, for solutionIntravenous15 mg/1mL
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US9636344No2017-05-022032-03-29US flag
US8466283No2013-06-182029-10-22US flag
US7511041No2009-03-312024-05-13US flag
USRE46856No2018-05-222029-10-22US flag
US10383876No2019-08-202032-03-29US flag

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.231 mg/mLALOGPS
logP1.02ALOGPS
logP0.32Chemaxon
logS-3.3ALOGPS
pKa (Strongest Acidic)10.15Chemaxon
pKa (Strongest Basic)6.88Chemaxon
Physiological Charge1Chemaxon
Hydrogen Acceptor Count11Chemaxon
Hydrogen Donor Count2Chemaxon
Polar Surface Area139.79 Å2Chemaxon
Rotatable Bond Count7Chemaxon
Refractivity132.78 m3·mol-1Chemaxon
Polarizability51.71 Å3Chemaxon
Number of Rings5Chemaxon
Bioavailability1Chemaxon
Rule of FiveNoChemaxon
Ghose FilterNoChemaxon
Veber's RuleNoChemaxon
MDDR-like RuleYesChemaxon
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/MSsplash10-001i-0300900000-bae1d15bd596281ff7ba
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSsplash10-056r-0007900000-857ba35577042f590c14
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSsplash10-004i-0104900000-7f9b89d528c93d2331a8
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSsplash10-001i-0401900000-2ae9b9abb943a2260cee
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSsplash10-0uei-2503900000-97de1a0645cb64d04cd7
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSsplash10-052r-2319300000-780a15f71bde0cb1ed99
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]-232.6020052
predicted
DarkChem Lite v0.1.0
[M-H]-204.10176
predicted
DeepCCS 1.0 (2019)
[M+H]+232.0984052
predicted
DarkChem Lite v0.1.0
[M+H]+206.45975
predicted
DeepCCS 1.0 (2019)
[M+Na]+233.6617052
predicted
DarkChem Lite v0.1.0
[M+Na]+212.5529
predicted
DeepCCS 1.0 (2019)

Targets

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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. Mensah FA, Blaize JP, Bryan LJ: Spotlight on copanlisib and its potential in the treatment of relapsed/refractory follicular lymphoma: evidence to date. Onco Targets Ther. 2018 Aug 13;11:4817-4827. doi: 10.2147/OTT.S142264. eCollection 2018. [Article]
  2. Markham A: Copanlisib: First Global Approval. Drugs. 2017 Dec;77(18):2057-2062. doi: 10.1007/s40265-017-0838-6. [Article]
  3. FDA Approved Drug Products: ALIQOPA (copanlisib) for injection, for intravenous use (September 2023) [Link]
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
  1. Mensah FA, Blaize JP, Bryan LJ: Spotlight on copanlisib and its potential in the treatment of relapsed/refractory follicular lymphoma: evidence to date. Onco Targets Ther. 2018 Aug 13;11:4817-4827. doi: 10.2147/OTT.S142264. eCollection 2018. [Article]
  2. Markham A: Copanlisib: First Global Approval. Drugs. 2017 Dec;77(18):2057-2062. doi: 10.1007/s40265-017-0838-6. [Article]
  3. FDA Approved Drug Products: ALIQOPA (copanlisib) for injection, for intravenous use (September 2023) [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Phosphatidylinositol-4,5-bisphosphate 3-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
PIK3CB
Uniprot ID
P42338
Uniprot Name
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform
Molecular Weight
122761.225 Da
References
  1. Markham A: Copanlisib: First Global Approval. Drugs. 2017 Dec;77(18):2057-2062. doi: 10.1007/s40265-017-0838-6. [Article]
  2. Mensah FA, Blaize JP, Bryan LJ: Spotlight on copanlisib and its potential in the treatment of relapsed/refractory follicular lymphoma: evidence to date. Onco Targets Ther. 2018 Aug 13;11:4817-4827. doi: 10.2147/OTT.S142264. eCollection 2018. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Protein serine/threonine kinase activity
Specific Function
Phosphoinositide-3-kinase (PI3K) that phosphorylates PtdIns(4,5)P2 (Phosphatidylinositol 4,5-bisphosphate) to generate phosphatidylinositol 3,4,5-trisphosphate (PIP3). PIP3 plays a key role by recr...
Gene Name
PIK3CG
Uniprot ID
P48736
Uniprot Name
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
Molecular Weight
126452.625 Da
References
  1. Markham A: Copanlisib: First Global Approval. Drugs. 2017 Dec;77(18):2057-2062. doi: 10.1007/s40265-017-0838-6. [Article]
  2. Mensah FA, Blaize JP, Bryan LJ: Spotlight on copanlisib and its potential in the treatment of relapsed/refractory follicular lymphoma: evidence to date. Onco Targets Ther. 2018 Aug 13;11:4817-4827. doi: 10.2147/OTT.S142264. eCollection 2018. [Article]

Enzymes

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
  1. FDA Approved Drug Products: ALIQOPA (copanlisib) for injection, for intravenous use (September 2023) [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
  1. FDA Approved Drug Products: ALIQOPA (copanlisib) for injection, for intravenous use (September 2023) [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
CYP3A7
Uniprot ID
P24462
Uniprot Name
Cytochrome P450 3A7
Molecular Weight
57525.03 Da
References
  1. FDA Approved Drug Products: ALIQOPA (copanlisib) for injection, for intravenous use (September 2023) [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
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
  1. FDA Approved Drug Products: ALIQOPA (copanlisib) for injection, for intravenous use (September 2023) [Link]

Carriers

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
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
  1. FDA Approved Drug Products: ALIQOPA (copanlisib) for injection, for intravenous use (September 2023) [Link]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
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
References
  1. FDA Approved Drug Products: ALIQOPA (copanlisib) for injection, for intravenous use (September 2023) [Link]
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. FDA Approved Drug Products: ALIQOPA (copanlisib) for injection, for intravenous use (September 2023) [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
Curator comments
At clinically significant concentrations, this drug does not inhibit MATE2. However, in vitro studies have shown inhibition and supratherapeutic doses.
General Function
Drug transmembrane transporter activity
Specific Function
Solute transporter for tetraethylammonium (TEA), 1-methyl-4-phenylpyridinium (MPP), cimetidine, N-methylnicotinamide, metformin, creatinine, guanidine, procainamide, topotecan, estrone sulfate, acy...
Gene Name
SLC47A2
Uniprot ID
Q86VL8
Uniprot Name
Multidrug and toxin extrusion protein 2
Molecular Weight
65083.915 Da
References
  1. Kim RD, Alberts SR, Pena C, Genvresse I, Ajavon-Hartmann A, Xia C, Kelly A, Grilley-Olson JE: Phase I dose-escalation study of copanlisib in combination with gemcitabine or cisplatin plus gemcitabine in patients with advanced cancer. Br J Cancer. 2018 Feb 20;118(4):462-470. doi: 10.1038/bjc.2017.428. Epub 2018 Jan 18. [Article]
  2. FDA Approved Drug Products: ALIQOPA (copanlisib) for injection, for intravenous use (September 2023) [Link]
  3. Copanlisib FDA label [File]

Drug created at October 20, 2016 22:33 / Updated at February 22, 2024 22:04