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

Similar Structures

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

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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 Type	Indication	Combined Product Details	Approval Level	Age Group	Patient Characteristics	Dose Form
Treatment of	Relapsed 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

Target	Actions	Organism
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 (C_max) 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 C_max and 1570 (range: 536 to 3410; SD: 338) ng x hr/mL for AUC_0-25h.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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Copanlisib

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

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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
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Abametapir	The serum concentration of Copanlisib can be increased when it is combined with Abametapir.
Abatacept	The metabolism of Copanlisib can be increased when combined with Abatacept.
Abemaciclib	Abemaciclib may decrease the excretion rate of Copanlisib which could result in a higher serum level.
Acalabrutinib	The metabolism of Copanlisib can be decreased when combined with Acalabrutinib.
Acetaminophen	The 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

Ingredient	UNII	CAS	InChI Key
Copanlisib dihydrochloride	03ZI7RZ52O	1402152-13-9	STGQPVQAAFJJFX-UHFFFAOYSA-N
Copanlisib dihydrochloride hydrate	W421JK3CPA	1402152-46-8	PRZNRMHJLYLVBJ-UHFFFAOYSA-N

Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End	Region	Image
Aliqopa	Injection, powder, lyophilized, for solution	15 mg/1mL	Intravenous	Bayer HealthCare Pharmaceuticals Inc.	2017-09-14	Not applicable

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

Markham A: Copanlisib: First Global Approval. Drugs. 2017 Dec;77(18):2057-2062. doi: 10.1007/s40265-017-0838-6. [Article]
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]
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]
FDA Press Announcements: FDA approves new treatment for adults with relapsed follicular lymphoma [Link]
FDA Approved Drug Products: ALIQOPA (copanlisib) for injection, for intravenous use (September 2023) [Link]
EMA: Aliqopa (copanlisib) withdrawal assessment report [Link]

External Links

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 Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">

Phase	Status	Purpose	Conditions	Count
3	Active Not Recruiting	Treatment	Non-Hodgkin's Lymphoma (NHL)	1
3	Completed	Treatment	Non-Hodgkin's Lymphoma (NHL)	1
3	Terminated	Treatment	Non-Hodgkin's Lymphoma (NHL)	1
2	Active Not Recruiting	Screening	Advanced 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 Cancer	1
2	Active Not Recruiting	Treatment	Advanced Lymphomas / Advanced Malignant Solid Tumor / Hematopoietic and Lymphoid System Neoplasm / Refractory Lymphomas / Refractory Malignant Solid Neoplasm / Refractory Multiple Myeloma	1

Pharmacoeconomics

Manufacturers

Not Available

Packagers

Not Available

Dosage Forms

Form	Route	Strength
Injection, powder, lyophilized, for solution	Intravenous	15 mg/1mL

Prices

Not Available

Patents

Patent Number	Pediatric Extension	Approved	Expires (estimated)
US9636344	No	2017-05-02	2032-03-29
US8466283	No	2013-06-18	2029-10-22
US7511041	No	2009-03-31	2024-05-13
USRE46856	No	2018-05-22	2029-10-22
US10383876	No	2019-08-20	2032-03-29

Properties

State

Solid

Experimental Properties

Not Available

Predicted Properties

Property	Value	Source
Water Solubility	0.231 mg/mL	ALOGPS
logP	1.02	ALOGPS
logP	0.32	Chemaxon
logS	-3.3	ALOGPS
pKa (Strongest Acidic)	10.15	Chemaxon
pKa (Strongest Basic)	6.88	Chemaxon
Physiological Charge	1	Chemaxon
Hydrogen Acceptor Count	11	Chemaxon
Hydrogen Donor Count	2	Chemaxon
Polar Surface Area	139.79 Å²	Chemaxon
Rotatable Bond Count	7	Chemaxon
Refractivity	132.78 m³·mol^-1	Chemaxon
Polarizability	51.71 Å³	Chemaxon
Number of Rings	5	Chemaxon
Bioavailability	1	Chemaxon
Rule of Five	No	Chemaxon
Ghose Filter	No	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, Positive (Annotated)	Predicted LC-MS/MS	splash10-001i-0300900000-bae1d15bd596281ff7ba
Predicted MS/MS Spectrum - 10V, Negative (Annotated)	Predicted LC-MS/MS	splash10-056r-0007900000-857ba35577042f590c14
Predicted MS/MS Spectrum - 20V, Negative (Annotated)	Predicted LC-MS/MS	splash10-004i-0104900000-7f9b89d528c93d2331a8
Predicted MS/MS Spectrum - 20V, Positive (Annotated)	Predicted LC-MS/MS	splash10-001i-0401900000-2ae9b9abb943a2260cee
Predicted MS/MS Spectrum - 40V, Positive (Annotated)	Predicted LC-MS/MS	splash10-0uei-2503900000-97de1a0645cb64d04cd7
Predicted MS/MS Spectrum - 40V, Negative (Annotated)	Predicted LC-MS/MS	splash10-052r-2319300000-780a15f71bde0cb1ed99
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]-	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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Details1. Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform

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

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]
Markham A: Copanlisib: First Global Approval. Drugs. 2017 Dec;77(18):2057-2062. doi: 10.1007/s40265-017-0838-6. [Article]
FDA Approved Drug Products: ALIQOPA (copanlisib) for injection, for intravenous use (September 2023) [Link]

Details2. Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform

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

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]
Markham A: Copanlisib: First Global Approval. Drugs. 2017 Dec;77(18):2057-2062. doi: 10.1007/s40265-017-0838-6. [Article]
FDA Approved Drug Products: ALIQOPA (copanlisib) for injection, for intravenous use (September 2023) [Link]

Details3. Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform

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

Markham A: Copanlisib: First Global Approval. Drugs. 2017 Dec;77(18):2057-2062. doi: 10.1007/s40265-017-0838-6. [Article]
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]

Details4. Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform

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

Markham A: Copanlisib: First Global Approval. Drugs. 2017 Dec;77(18):2057-2062. doi: 10.1007/s40265-017-0838-6. [Article]
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

Details1. Cytochrome P450 3A4

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

FDA Approved Drug Products: ALIQOPA (copanlisib) for injection, for intravenous use (September 2023) [Link]

Details2. Cytochrome P450 3A5

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: ALIQOPA (copanlisib) for injection, for intravenous use (September 2023) [Link]

Details3. Cytochrome P450 3A7

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

FDA Approved Drug Products: ALIQOPA (copanlisib) for injection, for intravenous use (September 2023) [Link]

Details4. Cytochrome P450 1A1

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

FDA Approved Drug Products: ALIQOPA (copanlisib) for injection, for intravenous use (September 2023) [Link]

Carriers

Details1. Serum albumin

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

FDA Approved Drug Products: ALIQOPA (copanlisib) for injection, for intravenous use (September 2023) [Link]

Transporters

Details1. P-glycoprotein 1

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

FDA Approved Drug Products: ALIQOPA (copanlisib) for injection, for intravenous use (September 2023) [Link]

Details2. ATP-binding cassette sub-family G member 2

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

FDA Approved Drug Products: ALIQOPA (copanlisib) for injection, for intravenous use (September 2023) [Link]

Details3. Multidrug and toxin extrusion protein 2

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

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]
FDA Approved Drug Products: ALIQOPA (copanlisib) for injection, for intravenous use (September 2023) [Link]
Copanlisib FDA label [File]

Drug created at October 20, 2016 22:33 / Updated at February 20, 2024 23:31

Copanlisib

Identification

Structure for Copanlisib (DB12483)

Pharmacology

Interactions

Products

Categories

Chemical Identifiers

References

Clinical Trials

Pharmacoeconomics

Properties

Spectra

Collision Cross Sections (CCS)

Targets

References

References

References

References

Enzymes

References

References

References

References

Carriers

References

Transporters

References

References

References