Copanlisib (Aliqopa)

Other Medications · Approved since 2017

US Off-label EU EMA Approved ES Hospital use other indication IV 2 Clinical Trials
PI3K-alpha PI3K-delta PI3K-beta PI3K-gamma

Description

Copanlisib is a pan-class I phosphoinositide 3-kinase (PI3K) inhibitor that targets the PI3K/AKT/mTOR signaling pathway. In colorectal cancer, it has been evaluated in combination with immunotherapy agents like nivolumab, particularly in microsatellite stable (MSS) tumors that typically respond poorly to immune checkpoint inhibitors alone. The drug aims to enhance immune response by modulating the tumor microenvironment through PI3K pathway inhibition.

Mechanism of Action

Copanlisib selectively inhibits class I PI3K isoforms, with particular potency against PI3K-alpha and PI3K-delta. By blocking PI3K signaling, it reduces AKT activation and downstream mTOR activity, leading to decreased tumor cell proliferation and survival while potentially enhancing T-cell infiltration and activity within the tumor microenvironment.

Molecular Targets

Side Effects

Hyperglycemia Hypertension Diarrhea Fatigue Nausea Decreased appetite Upper respiratory tract infection Rash

Not all side effects are listed. Side effects vary by individual. Always consult your oncologist.

Clinical Trials

NCT03711058 Phase 1
Completed
Study of PI3Kinase Inhibition (Copanlisib) and Anti-PD-1 Antibody Nivolumab in Relapsed/Refractory Solid Tumors With Expansions in Mismatch-repair Proficient (MSS) Colorectal Cancer
United States
NCT02465060 Phase 2
Active, not recruiting
Targeted Therapy Directed by Genetic Testing in Treating Patients With Advanced Refractory Solid Tumors, Lymphomas, or Multiple Myeloma (The MATCH Screening Trial)
United States, Guam, Puerto Rico