Copanlisib dihydrochloride

Copanlisib dihydrochloride
File:Copanlisib structure.png
INN
Drug class
Routes of administration	Intravenous
Pregnancy category
Bioavailability
Metabolism	Hepatic
Elimination half-life	39.1 hours
Excretion	Feces (64%), urine (22%)
Legal status
CAS Number	1038935-63-3
PubChem	25142104
DrugBank	DB12556
ChemSpider	32700806
KEGG	D10850

Copanlisib dihydrochloride is a pharmaceutical drug used in the treatment of certain types of cancer, specifically relapsed follicular lymphoma. It is a phosphoinositide 3-kinase (PI3K) inhibitor that targets the PI3K pathway, which is often dysregulated in cancer cells.

Mechanism of Action

Copanlisib is a selective inhibitor of the PI3K enzyme, particularly the PI3K-α and PI3K-δ isoforms. The PI3K pathway is involved in cellular functions such as growth, proliferation, and survival. By inhibiting this pathway, copanlisib can induce apoptosis and inhibit the proliferation of cancer cells.

Pharmacokinetics

Copanlisib is administered intravenously, allowing for direct entry into the bloodstream. It has a half-life of approximately 39.1 hours, which supports its dosing schedule. The drug is primarily metabolized in the liver and is excreted through feces (64%) and urine (22%).

Clinical Use

Copanlisib is approved for the treatment of adult patients with relapsed follicular lymphoma who have received at least two prior systemic therapies. It is administered as an intravenous infusion on a weekly basis, with a schedule of three weeks on treatment followed by one week off.

Adverse Effects

Common adverse effects of copanlisib include hyperglycemia, hypertension, diarrhea, decreased general strength and energy, and leukopenia. Serious adverse effects can include severe infections, pneumonitis, and severe cutaneous reactions.

Contraindications

Copanlisib is contraindicated in patients with a known hypersensitivity to the drug or any of its components. Caution is advised in patients with a history of severe infections or those with uncontrolled diabetes or hypertension.

Drug Interactions

Copanlisib may interact with other drugs that affect the cytochrome P450 enzyme system, particularly CYP3A4 inhibitors and inducers. Patients should be monitored for potential interactions that could affect the efficacy or toxicity of copanlisib.

Research and Development

Ongoing research is exploring the use of copanlisib in other types of cancer, including chronic lymphocytic leukemia and solid tumors. Clinical trials are investigating its efficacy in combination with other anticancer agents.

Regulatory Status

Copanlisib was granted accelerated approval by the U.S. Food and Drug Administration (FDA) in 2017 for the treatment of relapsed follicular lymphoma. It is marketed under the trade name Aliqopa.

See Also

• Phosphoinositide 3-kinase inhibitors
• Follicular lymphoma
• Cancer treatment

External Links

• [FDA Drug Information on Copanlisib]
• [Clinical Trials on Copanlisib]