Aliqopa

>10%

Any grade

• Hyperglycemia (54-95%)
• Decreased hemoglobin and lymphocytes (78%)
• Decreased white blood cells (WBCs) (71%)
• Decreased platelets (65%)
• Decreased neutrophils (63%)
• Hypertriglyceridemia (58%)
• Hypophosphatemia (44%)
• Leukopenia (36%)
• Decreased general strength and energy (36%)
• Diarrhea (36%)
• Hypertension (35%)
• Neutropenia (32%)
• Nausea (26%)
• Hyperuricemia (25%)
• Thrombocytopenia (22%)

Grade 3

• Hyperglycemia (43%)
• Decreased lymphocytes (27%)
• Hypertension (27%)
• Hyperuricemia (24%)
• Decreased WBCs (18%)
• Hyperphosphatemia (15%)
• Leukopenia (12%)
• Lower respiratory tract infections (12%)
• Decreased neutrophils (12%)

Grade 4

• Leukopenia (15%)
• Neutropenia (15%)

1-10%

Pneumonitis (9%)

Mucosal inflammation (8%)

Paresthesia and dysesthesia (7%)

Grade 3

• Neutropenia (10%)
• Thrombocytopenia (7%)
• Serum lipase increased (7%)
• Decreased platelets (7%)
• Hypertriglyceridemia (5%)
• Diarrhea (5%)
• Decreased general strength and energy (4%)
• Decreased hemoglobin (4%)
• Stomatitis (2%)
• Rash (1%)

Grade 4

• Hyperglycemia (5%)
• Lower respiratory tract infections (2%)
• Decreased lymphocytes (2%)
• Decreased WBCs (2%)
• Decreased platelets (2%)
• Thrombocytopenia (1%)
• Hyperuricemia (1%)
• Serum lipase increased (1%)

<1%

Nausea, grade 3

Rash, grade 4

Contraindications

None

Cautions

Serious, including fatal, infections may occur; the most common serious infection was pneumonia; monitor patients for signs/symptoms of infection and withhold treatment for grade 3 and higher infection

Grade 3 or 4 hyperglycemia (blood glucose 250 mg/dL or greater) reported; achieve optimal blood glucose control before starting each infusion; withhold, reduce dose, or discontinue treatment depending on the severity and persistence of hyperglycemia

Grade 3 hypertension (systolic 160 mm Hg or greater or diastolic 100 mm Hg or greater) may occur; optimal BP control should be achieved before starting each infusion; monitor BP preinfusion and postinfusion; withhold, reduce dose, or discontinue copanlisib depending on severity and persistence of hypertension

Noninfectious pneumonitis reported; withhold treatment and conduct a diagnostic examination of a patient who is experiencing pulmonary symptoms (eg, cough, dyspnea, hypoxia, interstitial infiltrates) on radiologic examination; withhold, reduce dose, or discontinue treatment depending on the severity and persistence of noninfectious pneumonitis

Grade 3 or 4 neutropenia may occur; withhold, reduce dose, or discontinue copanlisib depending on the severity and persistence of neutropenia

Serious cutaneous reaction events (eg, exfoliative dermatitis, exfoliative rash, pruritus, and rash [including maculopapular rash]) may occur; withhold, reduce dose, or discontinue treatment depending on the severity and persistence of severe cutaneous reactions

Advise females of reproductive potential and males with female partners of reproductive potential to use effective contraception during treatment and for at least 1 month after the last dose

Mechanism of Action

Pan class I phosphatidylinositol-3-kinase (PI3K) inhibitor with predominant inhibitory activity against PI3K-alpha and PI3K-delta isoforms expressed in malignant B cells; by inhibiting several key cell-signaling pathways may induce apoptosis and inhibition of proliferation of premalignant B cells and in turn cause tumor cell death

Absorption

Peak plasma concentration: 463 ng/mL

AUC (0-25): 1570 ng·hr/mL

Distribution

Protein binding: 84.2% (mainly albumin)

Vd: 871 L

Metabolism

Metabolism is mediated by CYP3A (~90%) and CYP1A1 (<10%)

Elimination

Half-life: 39.1 hr Clearance: 17.9 L/hr

Excreted ~50% as unchanged compound and 50% as metabolites

Excretion, unchanged compound: Feces (30%), urine (15%)

Aliqopa (copanlisib) is a cancer medicine that interferes with the growth and spread of cancer cells in the body.

Aliqopa is used to treat follicular lymphoma that has relapsed after treatment with at least two other medicines.

Aliqopa was approved by the US Food and Drug Administration (FDA) on an "accelerated" basis. In clinical studies, people with follicular lymphoma responded to this medicine. However, further studies are needed.

Data not available.