Copanlisib

Kinase Inhibitor — ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Key facts

Copanlisib is an onp drug in the Kinase Inhibitor class catalogued in DrugCentral. It was first approved by the FDA in 2017. Its mechanism of action is classified as Kinase Inhibitors. DrugCentral lists 6 molecular targets, including PIK3CA, PIK3CD and PIK3CB. Recorded indications include Follicular lymphoma.

• Approval status: onp (first approved 2017 by the FDA).
• Drug class: Kinase Inhibitor.
• Mechanism of action: Kinase Inhibitors.
• Molecular targets: PIK3CA, PIK3CD, PIK3CB and PIK3CG (6 listed in DrugCentral).
• Indications: Follicular lymphoma.
• ATC code: L01EM02 (Phosphatidylinositol-3-kinase (Pi3K) inhibitors).
• Molecular formula: C23H28N8O4; molecular weight 480.53 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (1)

• Follicular lymphoma

Mechanism & targets

• Mechanism of action (MoA): Kinase Inhibitors
• Established pharmacologic class: Kinase Inhibitor

Molecular targets (6)

Target	Gene	Action	Activity
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform	PIK3CA	inhibitor	IC50 9.30
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	PIK3CD	inhibitor	IC50 9.15
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform	PIK3CB	inhibitor	IC50 8.43
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform	PIK3CG	inhibitor	IC50 8.19
Serine/threonine-protein kinase mTOR	MTOR	inhibitor	IC50 7.35
Ras-related protein Rab-27A	RAB27A	unknown	Kd 5.35

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
2017-09-14	FDA	—	BAYER HEALTHCARE PHARMS	Yes

ATC classification

ATC code	Therapeutic hierarchy
L01EM02	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › PROTEIN KINASE INHIBITORS › Phosphatidylinositol-3-kinase (Pi3K) inhibitors

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Pyrexia	66.8
Rash maculo-papular	62.8
Neutropenic sepsis	62.5
Metastases to retroperitoneum	62.5
Metastases to muscle	62.1
Hyperglycaemia	57.6
Cytopenia	56.7
Metastases to spleen	55.7
Metastases to bone marrow	52.6
End stage renal disease	47.7

Chemical structure

• Molecular formula: C₂₃H₂₈N₈O₄
• Molecular weight: 480.53 g/mol
• CAS number: —
• InChIKey: PZBCKZWLPGJMAO-UHFFFAOYSA-N
• PubChem CID: 135565596

COC1=C(OCCCN2CCOCC2)C=CC2=C1N=C(NC(=O)C1=CN=C(N)N=C1)N1CCN=C21

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Copanlisib used for?

DrugCentral lists the following indications for Copanlisib: Follicular lymphoma.

How does Copanlisib work?

Copanlisib is classified as Kinase Inhibitors; its molecular targets in DrugCentral include PIK3CA (inhibitor), PIK3CD (inhibitor), PIK3CB (inhibitor) and PIK3CG (inhibitor).

When was Copanlisib first approved?

Copanlisib was first approved by the FDA in 2017.

What drug class does Copanlisib belong to?

Copanlisib is in the Kinase Inhibitor class.

What is the chemical formula of Copanlisib?

Copanlisib has the molecular formula C23H28N8O4 and a molecular weight of 480.53 g/mol.

Sources

• DrugCentral drug card 5256 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL3218576 — compound record and bioactivity
• PubChem CID 135565596 — chemical identifiers
• DrugBank DB12483 — drug record
• FDA UNII WI6V529FZ9 — substance identity
• DailyMed: FDA labels for Copanlisib — current prescribing information (label search)
• UniProt P42336 (PIK3CA) — target protein
• UniProt O00329 (PIK3CD) — target protein
• UniProt P42338 (PIK3CB) — target protein
• UniProt P48736 (PIK3CG) — target protein
• UniProt P42345 (MTOR) — target protein
• UniProt P51159 (RAB27A) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

How this page is built: methodology · editorial policy & corrections.