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Copanlisib: Drug information

Copanlisib: Drug information
(For additional information see "Copanlisib: Patient drug information")

For abbreviations, symbols, and age group definitions used in Lexicomp (show table)
Brand Names: US
  • Aliqopa
Pharmacologic Category
  • Antineoplastic Agent, Phosphatidylinositol 3-Kinase Inhibitor
Dosing: Adult
Follicular lymphoma

Follicular lymphoma (relapsed): IV: 60 mg on days 1, 8, and 15 of a 28-day treatment cycle; continue until disease progression or unacceptable toxicity (Dreyling 2017).

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Adult

Note: Renal function may be estimated using the Cockcroft-Gault formula.

CrCl ≥15 mL/minute: There are no dosage adjustments provided in the manufacturer's labeling; however, CrCl ≥15 mL/minute did not significantly affect the pharmacokinetics of copanlisib.

CrCl <15 mL/minute: There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).

End-stage renal disease with or without dialysis: There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).

Dosing: Hepatic Impairment: Adult

Mild impairment (total bilirubin ≤ ULN and AST > ULN or total bilirubin 1 to 1.5 times ULN and any AST): No dosage adjustment necessary.

Moderate impairment (Child-Pugh class B): Reduce dose to 45 mg.

Severe hepatic impairment (Child-Pugh class C): Reduce dose to 30 mg.

Dosing: Older Adult

Refer to adult dosing.

Dosing: Adjustment for Toxicity: Adult

Note: A minimum of 7 days should elapse between any 2 consecutive infusions. Manage toxicities with dose reduction, treatment delay, or therapy discontinuation.

Hematologic toxicity:

Neutropenia:

ANC 500 to 1,000/mm3: Continue current copanlisib dose; monitor ANC at least weekly.

ANC <500/mm3: Interrupt copanlisib therapy. Monitor ANC at least weekly until ≥500/mm3, then resume at the previous dose. If ANC <500/mm3 recurs, then reduce copanlisib dose to 45 mg.

Thrombocytopenia: Platelets <25,000/mm3: Interrupt copanlisib therapy. May resume treatment when platelets recover to ≥75,000/mm3; if recovery occurs within 21 days, reduce dose from 60 mg to 45 mg (or from 45 mg to 30 mg). If recovery does not occur within 21 days, discontinue copanlisib.

Nonhematologic toxicity:

Dermatologic toxicity:

Grade 3 cutaneous reaction: Interrupt copanlisib therapy until toxicity is resolved; upon recovery, reduce dose from 60 mg to 45 mg (or from 45 mg to 30 mg).

Life-threatening: Discontinue copanlisib

Hyperglycemia:

Pre-dose fasting blood glucose ≥160 mg/dL or random (non-fasting) blood glucose ≥200 mg/dL: Withhold copanlisib until fasting glucose is ≤160 mg/dL or a random (non-fasting) blood glucose is ≤200 mg/dL.

Pre-dose or post-dose blood glucose ≥500 mg/dL:

First occurrence: Withhold copanlisib until fasting blood glucose is ≤160 mg/dL, or a random (nonfasting) blood glucose is ≤200 mg/dL. Reduce dose from 60 mg to 45 mg.

Subsequent occurrences: Withhold copanlisib until fasting blood glucose is ≤160 mg/dL, or a random (nonfasting) blood glucose is ≤200 mg/dL. Reduce dose from 45 mg to 30 mg. If hyperglycemia is persistent at the 30 mg dose, discontinue copanlisib.

Hypertension:

Pre-dose blood pressure ≥150/90: Withhold copanlisib until blood pressure is <150/90 (both systolic and diastolic) based on 2 consecutive measurements at least 15 minutes apart.

Post-dose blood pressure ≥150/90 (not life-threatening): If antihypertensive therapy is not required, continue copanlisib at the previous dose. If antihypertensive treatment is necessary, consider copanlisib dose reduction from 60 mg to 45 mg (or from 45 mg to 30 mg). Discontinue copanlisib if blood pressure remains uncontrolled (>150/90) despite appropriate antihypertensive treatment.

Post-dose elevated blood pressure with life-threatening consequences: Discontinue copanlisib.

Infection:

≥ Grade 3: Withhold copanlisib until resolution of infection.

Suspected pneumocystis jirovecii pneumonia (PCP) infection of any grade: Withhold copanlisib; if infection is confirmed, treat infection until resolution, then resume copanlisib at previous dose with concomitant PCP prophylaxis.

Pneumonitis (noninfectious):

Grade 2: Withhold copanlisib and treat pneumonitis appropriately. If noninfectious pneumonitis recovers to grade 0 or 1, resume copanlisib at 45 mg. If grade 2 toxicity recurs, discontinue copanlisib.

≥ Grade 3: Discontinue copanlisib.

Other severe and non-life-threatening toxicities: Grade 3: Withhold copanlisib until resolution and reduce copanlisib from 60 mg to 45 mg (or from 45 mg to 30 mg).

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Solution Reconstituted, Intravenous:

Aliqopa: 60 mg (1 ea)

Generic Equivalent Available: US

No

Administration: Adult

IV: Infuse over 1 hour. Do not mix with or administer with any other medications. Do not infuse with any solutions other than NS.

Hazardous Drugs Handling Considerations

This medication is not on the NIOSH (2016) list; however, it may meet the criteria for a hazardous drug. Copanlisib may cause reproductive toxicity and teratogenicity.

Use appropriate precautions for receiving, handling, storage, preparation, dispensing, transporting, administration, and disposal. Follow NIOSH and USP 800 recommendations and institution-specific policies/procedures for appropriate containment strategy (NIOSH 2016; USP-NF 2020).

Note: Facilities may perform risk assessment of some hazardous drugs to determine if appropriate for alternative handling and containment strategies (USP-NF 2020). Refer to institution-specific handling policies/procedures.

Use: Labeled Indications

Follicular lymphoma (relapsed): Treatment of relapsed follicular lymphoma (FL) in adults who have received at least two prior systemic therapies

Medication Safety Issues
Sound-alike/look-alike issues:

Copanlisib may be confused with alpelisib, crizotinib, duvelisib, idelalisib

High alert medication:

This medication is in a class the Institute for Safe Medication Practices (ISMP) includes among its list of drug classes which have a heightened risk of causing significant patient harm when used in error.

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.

>10%:

Cardiovascular: Hypertension (35%)

Central nervous system: Fatigue (36%)

Dermatologic: Skin rash (15%)

Endocrine & metabolic: Hyperglycemia (54% to 95%), hypertriglyceridemia (58%), hypophosphatemia (44%), hyperuricemia (25%)

Gastrointestinal: Diarrhea (36%), nausea (26%), increased serum lipase (21%), stomatitis (14%), vomiting (13%)

Hematologic & oncologic: Decreased hemoglobin (78%; grade 3: 4%), leukopenia (36%; grade 3: 12%; grade 4: 15%), decreased absolute lymphocyte count (78%; grade 3: 27%; grade 4: 2%), neutropenia (32%; grade 3: 10% to ≤24%; grade 4: 15% to ≤24%), thrombocytopenia (22%; grade 3: 7%; grade 4: 1%)

Infection: Serious infection (19%)

Respiratory: Lower respiratory tract infection (21%)

1% to 10%:

Central nervous system: Dysesthesia (≤7%), paresthesia (≤7%)

Endocrine & metabolic: Severe hyperglycemia (3% to 5%)

Gastrointestinal: Mucosal inflammation (8%)

Hematologic & oncologic: Severe neutropenia (1%)

Respiratory: Pneumonitis (5% to 9%), pneumonia (8%)

<1%, postmarketing and/or case reports: Exfoliative dermatitis, pneumonia due to pneumocystis, pruritus

Contraindications

There are no contraindications listed in the manufacturer's labeling

Warnings/Precautions

Concerns related to adverse effects:

• Bone marrow suppression: Leukopenia, neutropenia, thrombocytopenia, lymphopenia, and anemia (including grade 3 or 4 events), have been reported with copanlisib therapy. Grade 3 or 4 neutropenia has occurred in close to one quarter of patients receiving copanlisib; serious neutropenic events also were reported. Monitor blood counts at least weekly during treatment; therapy interruption, dose reduction, or treatment discontinuation may be necessary depending on the severity and persistence of neutropenia.

• Dermatologic toxicity: Dermatologic toxicities, including grade 3 and 4 cutaneous events, have been observed with copanlisib monotherapy. Toxicities included exfoliative dermatitis, exfoliative rash, pruritus, and rash (including maculopapular rash). Therapy interruption, dose reduction, or treatment discontinuation may be necessary depending on the severity and persistence of severe cutaneous reactions.

• Hyperglycemia: Grade 3 or 4 hyperglycemia was reported commonly in patients treated with copanlisib monotherapy, including serious hyperglycemic events; infusion-related hyperglycemia may occur. Serum glucose levels typically peaked at 5 to 8 hours post infusion, and then declined to baseline levels in the majority of patients; some patients had elevated serum glucose levels one day after the infusion. In patients with baseline HbA1c <5.7%, 10% had HbA1c >6.5% at the conclusion of copanlisib therapy. Prior to each copanlisib infusion, achieve optimal serum glucose control; therapy interruption, dose reduction, or treatment discontinuation may be necessary depending on the severity and persistence of hyperglycemia. Patients with diabetes mellitus should only be treated with copanlisib if adequate glucose control is achieved; monitor closely.

• Hypertension: Hypertension (including grade 3 and serious events) has occurred during copanlisib therapy; infusion-related hypertension may occur. Grade 3 hypertension (systolic blood pressure ≥160 mm Hg or diastolic blood pressure ≥100 mm Hg) was reported in over one quarter of patients treated with copanlisib monotherapy. Systolic and diastolic blood pressures increased 16.8 mm Hg and 7.8 mm Hg, respectively, from baseline to 2 hours post infusion (in cycle 1 day 1); the mean blood pressure began decreasing ~2 hours post infusion, however, blood pressure remained elevated for 6 to 8 hours after the start of infusion. Monitor blood pressure before and after infusion; optimize blood pressure control prior to initiating each dose. Therapy interruption, dose reduction, or treatment discontinuation may be necessary depending on the severity and persistence of hypertension.

• Infection: Serious and fatal infections have occurred during treatment with copanlisib. The most commonly reported infection was pneumonia. Monitor for signs and symptoms of infection and interrupt therapy for grade 3 and higher infections. Serious Pneumocystis jirovecii pneumonia (PCP) has also been reported (rarely). Consider PCP prophylaxis in patients at risk; interrupt copanlisib for suspected PCP infection (any grade). If confirmed, treat infection until resolution and then resume copanlisib therapy at the previous dose (with concomitant PCP prophylaxis).

• Pulmonary toxicity: Noninfectious pneumonitis has been reported with copanlisib monotherapy. Interrupt treatment and determine cause in patients with pulmonary symptoms (eg, cough, dyspnea, hypoxia, or interstitial infiltrates on radiologic exam). Management for copanlisib-induced pneumonitis may include therapy interruption and systemic corticosteroids. Therapy interruption, dose reduction, or treatment discontinuation may be necessary depending on the severity and persistence of non-infectious pneumonitis.

Metabolism/Transport Effects

Substrate of BCRP/ABCG2, CYP3A4 (major), P-glycoprotein/ABCB1 (minor); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential

Drug Interactions

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.

5-Aminosalicylic Acid Derivatives: May enhance the myelosuppressive effect of Myelosuppressive Agents. Risk C: Monitor therapy

Abrocitinib: May enhance the immunosuppressive effect of Immunosuppressants (Miscellaneous Oncologic Agents). Risk X: Avoid combination

Androgens: Hypertension-Associated Agents may enhance the hypertensive effect of Androgens. Risk C: Monitor therapy

Antidiabetic Agents: Hyperglycemia-Associated Agents may diminish the therapeutic effect of Antidiabetic Agents. Risk C: Monitor therapy

Baricitinib: Immunosuppressants (Miscellaneous Oncologic Agents) may enhance the immunosuppressive effect of Baricitinib. Risk X: Avoid combination

BCG (Intravesical): Myelosuppressive Agents may diminish the therapeutic effect of BCG (Intravesical). Risk X: Avoid combination

BCG Products: Immunosuppressants (Miscellaneous Oncologic Agents) may enhance the adverse/toxic effect of BCG Products. Specifically, the risk of vaccine-associated infection may be increased. Immunosuppressants (Miscellaneous Oncologic Agents) may diminish the therapeutic effect of BCG Products. Risk X: Avoid combination

Brincidofovir: Immunosuppressants (Miscellaneous Oncologic Agents) may diminish the therapeutic effect of Brincidofovir. Risk C: Monitor therapy

Chloramphenicol (Ophthalmic): May enhance the adverse/toxic effect of Myelosuppressive Agents. Risk C: Monitor therapy

Cladribine: May enhance the myelosuppressive effect of Myelosuppressive Agents. Risk X: Avoid combination

Cladribine: Immunosuppressants (Miscellaneous Oncologic Agents) may enhance the immunosuppressive effect of Cladribine. Risk X: Avoid combination

Clofazimine: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy

CloZAPine: Myelosuppressive Agents may enhance the adverse/toxic effect of CloZAPine. Specifically, the risk for neutropenia may be increased. Risk C: Monitor therapy

Coccidioides immitis Skin Test: Immunosuppressants (Miscellaneous Oncologic Agents) may diminish the diagnostic effect of Coccidioides immitis Skin Test. Management: Consider discontinuing these oncologic agents several weeks prior to coccidioides immitis skin antigen testing to increase the likelihood of accurate diagnostic results. Risk D: Consider therapy modification

COVID-19 Vaccine (Adenovirus Vector): Immunosuppressants (Miscellaneous Oncologic Agents) may diminish the therapeutic effect of COVID-19 Vaccine (Adenovirus Vector). Management: Administer a 2nd dose using an mRNA COVID-19 vaccine (at least 4 weeks after the primary vaccine dose) and a bivalent booster dose (at least 2 months after the additional mRNA dose or any other boosters). Risk D: Consider therapy modification

COVID-19 Vaccine (Inactivated Virus): Immunosuppressants (Miscellaneous Oncologic Agents) may diminish the therapeutic effect of COVID-19 Vaccine (Inactivated Virus). Risk C: Monitor therapy

COVID-19 Vaccine (mRNA): Immunosuppressants (Miscellaneous Oncologic Agents) may diminish the therapeutic effect of COVID-19 Vaccine (mRNA). Management: Give a 3-dose primary series for all patients aged 6 months and older taking immunosuppressive medications or therapies. Booster doses are recommended for certain age groups. See CDC guidance for details. Risk D: Consider therapy modification

COVID-19 Vaccine (Subunit): Immunosuppressants (Miscellaneous Oncologic Agents) may diminish the therapeutic effect of COVID-19 Vaccine (Subunit). Risk C: Monitor therapy

COVID-19 Vaccine (Virus-like Particles): Immunosuppressants (Miscellaneous Oncologic Agents) may diminish the therapeutic effect of COVID-19 Vaccine (Virus-like Particles). Risk C: Monitor therapy

CYP3A4 Inducers (Moderate): May decrease the serum concentration of Copanlisib. Risk C: Monitor therapy

CYP3A4 Inducers (Strong): May decrease the serum concentration of Copanlisib. Risk X: Avoid combination

CYP3A4 Inhibitors (Moderate): May increase the serum concentration of Copanlisib. Risk C: Monitor therapy

CYP3A4 Inhibitors (Strong): May increase the serum concentration of Copanlisib. Management: If concomitant use of copanlisib and strong CYP3A4 inhibitors cannot be avoided, reduce the copanlisib dose to 45 mg. Monitor patients for increased copanlisib effects/toxicities. Risk D: Consider therapy modification

Deferiprone: Myelosuppressive Agents may enhance the neutropenic effect of Deferiprone. Management: Avoid the concomitant use of deferiprone and myelosuppressive agents whenever possible. If this combination cannot be avoided, monitor the absolute neutrophil count more closely. Risk D: Consider therapy modification

Dengue Tetravalent Vaccine (Live): Immunosuppressants (Miscellaneous Oncologic Agents) may enhance the adverse/toxic effect of Dengue Tetravalent Vaccine (Live). Specifically, the risk of vaccine-associated infection may be increased. Immunosuppressants (Miscellaneous Oncologic Agents) may diminish the therapeutic effect of Dengue Tetravalent Vaccine (Live). Risk X: Avoid combination

Denosumab: May enhance the immunosuppressive effect of Immunosuppressants (Miscellaneous Oncologic Agents). Management: Consider the risk of serious infections versus the potential benefits of coadministration of denosumab and immunosuppressants. If combined, monitor patients for signs/symptoms of serious infections. Risk D: Consider therapy modification

Deucravacitinib: May enhance the immunosuppressive effect of Immunosuppressants (Miscellaneous Oncologic Agents). Risk X: Avoid combination

Dipyrone: May enhance the adverse/toxic effect of Myelosuppressive Agents. Specifically, the risk for agranulocytosis and pancytopenia may be increased Risk X: Avoid combination

Fexinidazole: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk X: Avoid combination

Fexinidazole: Myelosuppressive Agents may enhance the myelosuppressive effect of Fexinidazole. Risk X: Avoid combination

Filgotinib: May enhance the immunosuppressive effect of Immunosuppressants (Miscellaneous Oncologic Agents). Risk X: Avoid combination

Fusidic Acid (Systemic): May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk X: Avoid combination

Inebilizumab: Immunosuppressants (Miscellaneous Oncologic Agents) may enhance the immunosuppressive effect of Inebilizumab. Risk C: Monitor therapy

Influenza Virus Vaccines: Immunosuppressants (Miscellaneous Oncologic Agents) may diminish the therapeutic effect of Influenza Virus Vaccines. Management: Administer influenza vaccines at least 2 weeks prior to initiating immunosuppressants if possible. If vaccination occurs less than 2 weeks prior to or during therapy, revaccinate at least 3 months after therapy discontinued if immune competence restored. Risk D: Consider therapy modification

Leflunomide: Immunosuppressants (Miscellaneous Oncologic Agents) may enhance the immunosuppressive effect of Leflunomide. Management: Increase the frequency of chronic monitoring of platelet, white blood cell count, and hemoglobin or hematocrit to monthly, instead of every 6 to 8 weeks, if leflunomide is coadministered with immunosuppressive agents. Risk D: Consider therapy modification

Natalizumab: Immunosuppressants (Miscellaneous Oncologic Agents) may enhance the immunosuppressive effect of Natalizumab. Risk X: Avoid combination

Ocrelizumab: Immunosuppressants (Miscellaneous Oncologic Agents) may enhance the immunosuppressive effect of Ocrelizumab. Risk C: Monitor therapy

Ofatumumab: Immunosuppressants (Miscellaneous Oncologic Agents) may enhance the immunosuppressive effect of Ofatumumab. Risk C: Monitor therapy

Olaparib: Myelosuppressive Agents may enhance the myelosuppressive effect of Olaparib. Risk C: Monitor therapy

Pidotimod: Immunosuppressants (Miscellaneous Oncologic Agents) may diminish the therapeutic effect of Pidotimod. Risk C: Monitor therapy

Pimecrolimus: May enhance the immunosuppressive effect of Immunosuppressants (Miscellaneous Oncologic Agents). Risk X: Avoid combination

Pneumococcal Vaccines: Immunosuppressants (Miscellaneous Oncologic Agents) may diminish the therapeutic effect of Pneumococcal Vaccines. Risk C: Monitor therapy

Poliovirus Vaccine (Live/Trivalent/Oral): Immunosuppressants (Miscellaneous Oncologic Agents) may enhance the adverse/toxic effect of Poliovirus Vaccine (Live/Trivalent/Oral). Specifically, the risk of vaccine-associated infection may be increased. Immunosuppressants (Miscellaneous Oncologic Agents) may diminish the therapeutic effect of Poliovirus Vaccine (Live/Trivalent/Oral). Risk X: Avoid combination

Polymethylmethacrylate: Immunosuppressants (Miscellaneous Oncologic Agents) may enhance the potential for allergic or hypersensitivity reactions to Polymethylmethacrylate. Management: Use caution when considering use of bovine collagen-containing implants such as the polymethylmethacrylate-based Bellafill brand implant in patients who are receiving immunosuppressants. Consider use of additional skin tests prior to administration. Risk D: Consider therapy modification

Promazine: May enhance the myelosuppressive effect of Myelosuppressive Agents. Risk C: Monitor therapy

Rabies Vaccine: Immunosuppressants (Miscellaneous Oncologic Agents) may diminish the therapeutic effect of Rabies Vaccine. Management: Complete rabies vaccination at least 2 weeks before initiation of immunosuppressant therapy if possible. If combined, check for rabies antibody titers, and if vaccination is for post exposure prophylaxis, administer a 5th dose of the vaccine. Risk D: Consider therapy modification

Ropeginterferon Alfa-2b: Myelosuppressive Agents may enhance the myelosuppressive effect of Ropeginterferon Alfa-2b. Management: Avoid coadministration of ropeginterferon alfa-2b and other myelosuppressive agents. If this combination cannot be avoided, monitor patients for excessive myelosuppressive effects. Risk D: Consider therapy modification

Rubella- or Varicella-Containing Live Vaccines: May enhance the adverse/toxic effect of Immunosuppressants (Miscellaneous Oncologic Agents). Specifically, the risk of vaccine-associated infection may be increased. Immunosuppressants (Miscellaneous Oncologic Agents) may diminish the therapeutic effect of Rubella- or Varicella-Containing Live Vaccines. Risk X: Avoid combination

Ruxolitinib (Topical): Immunosuppressants (Miscellaneous Oncologic Agents) may enhance the immunosuppressive effect of Ruxolitinib (Topical). Risk X: Avoid combination

Sipuleucel-T: Immunosuppressants (Miscellaneous Oncologic Agents) may diminish the therapeutic effect of Sipuleucel-T. Management: Consider reducing the dose or discontinuing the use of immunosuppressants prior to initiating sipuleucel-T therapy. Risk D: Consider therapy modification

Solriamfetol: May enhance the hypertensive effect of Hypertension-Associated Agents. Risk C: Monitor therapy

Sphingosine 1-Phosphate (S1P) Receptor Modulator: May enhance the immunosuppressive effect of Immunosuppressants (Miscellaneous Oncologic Agents). Risk C: Monitor therapy

Tacrolimus (Topical): Immunosuppressants (Miscellaneous Oncologic Agents) may enhance the immunosuppressive effect of Tacrolimus (Topical). Risk X: Avoid combination

Talimogene Laherparepvec: Immunosuppressants (Miscellaneous Oncologic Agents) may enhance the adverse/toxic effect of Talimogene Laherparepvec. Specifically, the risk of infection from the live, attenuated herpes simplex virus contained in talimogene laherparepvec may be increased. Risk X: Avoid combination

Tertomotide: Immunosuppressants (Miscellaneous Oncologic Agents) may diminish the therapeutic effect of Tertomotide. Risk X: Avoid combination

Tofacitinib: Immunosuppressants (Miscellaneous Oncologic Agents) may enhance the immunosuppressive effect of Tofacitinib. Risk X: Avoid combination

Typhoid Vaccine: Immunosuppressants (Miscellaneous Oncologic Agents) may enhance the adverse/toxic effect of Typhoid Vaccine. Specifically, the risk of vaccine-associated infection may be increased. Immunosuppressants (Miscellaneous Oncologic Agents) may diminish the therapeutic effect of Typhoid Vaccine. Risk X: Avoid combination

Upadacitinib: Immunosuppressants (Miscellaneous Oncologic Agents) may enhance the immunosuppressive effect of Upadacitinib. Risk X: Avoid combination

Vaccines (Inactivated/Non-Replicating): Immunosuppressants (Miscellaneous Oncologic Agents) may diminish the therapeutic effect of Vaccines (Inactivated/Non-Replicating). Management: Give inactivated vaccines at least 2 weeks prior to initiation of immunosuppressants when possible. Patients vaccinated less than 14 days before initiating or during therapy should be revaccinated at least 3 after therapy is complete. Risk D: Consider therapy modification

Vaccines (Live): Immunosuppressants (Miscellaneous Oncologic Agents) may enhance the adverse/toxic effect of Vaccines (Live). Specifically, the risk of vaccine-associated infection may be increased. Immunosuppressants (Miscellaneous Oncologic Agents) may diminish the therapeutic effect of Vaccines (Live). Risk X: Avoid combination

Yellow Fever Vaccine: Immunosuppressants (Miscellaneous Oncologic Agents) may enhance the adverse/toxic effect of Yellow Fever Vaccine. Specifically, the risk of vaccine-associated infection may be increased. Immunosuppressants (Miscellaneous Oncologic Agents) may diminish the therapeutic effect of Yellow Fever Vaccine. Risk X: Avoid combination

Food Interactions

Grapefruit juice may increase serum copanlisib levels.

Reproductive Considerations

Pregnancy testing should be conducted prior to therapy in women of reproductive potential. Highly effective contraception (contraception with a failure rate of <1% per year) is recommended in women of reproductive potential during treatment and for at least 1 month after the last dose. Males with female partners of reproductive potential should also use highly effective contraception during treatment and for at least 1 month after the last copanlisib dose.

Pregnancy Considerations

Based on the mechanism of action and data from animal reproduction studies, in utero exposure to copanlisib may cause fetal harm.

Breastfeeding Considerations

It is not known if copanlisib is present in breast milk. Due to the potential for serious adverse events in the breastfed infant, the manufacturer does not recommend breastfeeding during therapy and for at least 1 month after treatment is discontinued.

Monitoring Parameters

Monitor blood counts at least weekly during treatment; blood glucose and BP pre-and post-dose and more frequently if clinically indicated; pregnancy test (prior to treatment in in females of reproductive potential); monitor for signs/symptoms of infection (eg, pneumocystis jirovecii pneumonia), non-infectious pneumonitis, and dermatologic toxicity.

The American Society of Clinical Oncology hepatitis B virus (HBV) screening and management provisional clinical opinion (ASCO [Hwang 2020]) recommends HBV screening with hepatitis B surface antigen, hepatitis B core antibody, total Ig or IgG, and antibody to hepatitis B surface antigen prior to beginning (or at the beginning of) systemic anticancer therapy; do not delay treatment for screening/results. Detection of chronic or past HBV infection requires a risk assessment to determine antiviral prophylaxis requirements, monitoring, and follow-up.

Mechanism of Action

Copanlisib inhibits phosphatidylinositol 3-kinase (PI3K), primarily the P13K-alpha and P13K-delta isoforms which are expressed in malignant B-cells. Copanlisib induces tumor cell death through apoptosis and inhibition of proliferation of primary malignant B cell lines. In addition, copanlisib inhibits several signaling pathways, including B-cell receptor signaling, CXCR12 mediated chemotaxis of malignant B cells, and NFκB signaling in lymphoma cell lines.

Pharmacokinetics

Distribution: 871 L (range: 423 to 2,150 L)

Protein binding: 84.2%, primarily to albumin

Metabolism: Primarily hepatic (>90%) though CYP3A and <10% through CYP1A1; the M-1 metabolite has pharmacologic activity comparable to the parent compound (against P13K-alpha and P13K-beta)

Half-life elimination: 39.1 hours (range: 14.6 to 82.4 hours)

Excretion: 12 mg IV dose: Feces (~64%; ~30% as unchanged drug); urine (~22%; ~15% as unchanged drug); metabolites account for 41% of the administered dose

Pharmacokinetics: Additional Considerations

Hepatic function impairment: In a pharmacokinetic study evaluating a single 12 mg IV copanlisib dose in subjects with hepatic impairment, the geometric mean of total copanlisib Cmax and AUC increased 1.38- and 1.71-fold, respectively, in subjects with moderate impairment (Child-Pugh class B) and 1.44- and 2.71-fold, respectively, in subjects with severe impairment (Child-Pugh class C) when compared to subjects with normal hepatic function. The geometric mean unbound AUC of copanlisib was increased by 1.23-fold and 3.77-fold in patients with moderate and severe impairment, respectively (with no effect on Cmax).

Pricing: US

Solution (reconstituted) (Aliqopa Intravenous)

60 mg (per each): $5,940.72

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Brand Names: International
  • Aliqopa (IN, TW)


For country code abbreviations (show table)
  1. <800> Hazardous Drugs—Handling in Healthcare Settings. United States Pharmacopeia and National Formulary (USP 43-NF 38). Rockville, MD: United States Pharmacopeia Convention; 2020:74-92.
  2. Aliqopa (copanlisib) [prescribing information]. Whippany, NJ: Bayer Healthcare Pharmaceuticals Inc; February 2022.
  3. Dreyling M, Santoro A, Mollica L, et al. Phosphatidylinositol 3-kinase inhibition by copanlisib in relapsed or refractory indolent lymphoma. J Clin Oncol. 2017;35(35):3898-3905. doi:10.1200/JCO.2017.75.4648 [PubMed 28976790]
  4. Hwang JP, Feld JJ, Hammond SP, et al. Hepatitis B virus screening and management for patients with cancer prior to therapy: ASCO provisional clinical opinion update. J Clin Oncol. 2020;38(31):3698-3715. doi:10.1200/JCO.20.01757 [PubMed 32716741]
  5. US Department of Health and Human Services; Centers for Disease Control and Prevention; National Institute for Occupational Safety and Health. NIOSH list of antineoplastic and other hazardous drugs in healthcare settings 2016. https://www.cdc.gov/niosh/docs/2016-161/. Updated September 2016. Accessed September 18, 2017.
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