copanlisib (Rx)

Brand and Other Names:Aliqopa
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

injection, lyophilized powder for reconstitution

  • 60 mg (single dose)

Follicular Lymphoma

Indicated for relapsed follicular lymphoma (FL) in patients who have received at least 2 prior systemic therapies

60 mg IV on Days 1, 8, and 15 of a 28-day treatment cycle on an intermittent schedule (21 days on and 7 days off)

Continue treatment until disease progression or unacceptable toxicity

Dosage Modifications

Coadministration of CYP3A4 inducers or inhibitors

Avoid concomitant use with strong CYP3A inducers

Concomitant use with strong CYP3A4 inhibitors: Reduce copanlisib dose to 45 mg

Infections

  • Grade ≥3: Withhold until resolution
  • Suspected pneumocystis jiroveci pneumonia (PJP) infection (all grades): Withhold treatment; if confirmed, treat infection until resolution, and then resume treatment at previous dose with concomitant PJP prophylaxis

Hyperglycemia

  • Predose fasting blood glucose (FBG) ≥160 mg/dL or random/non-FBG ≥200 mg/dL: Withhold treatment until predose FBG ≤160 mg/dL or random/non-FBG ≤200 mg/dL
  • Predose or postdose blood glucose ≥500 mg/dL
    • First occurrence: Withhold treatment until FBG is ≤160 mg/dL, or a random/non-FBG ≤200 mg/dL; then reduce dose from 60 mg to 45 mg and maintain at 45 mg
    • Subsequent occurrences: Withhold treatment until FBG is ≤160 mg/dL, or a random/non-FBG ≤200 mg/dL; then reduce dose from 45 mg to 30 mg and maintain at 30 mg
    • Discontinue treatment if it persists at 30 mg

Hypertension

  • Predose blood pressure (BP) ≥150/90 mm Hg: Withhold treatment until BP <150/90 mm Hg based on 2 consecutive BP measurements at least 15 minutes apart
  • Postdose elevated BP with life-threatening consequences: Discontinue treatment
  • Non-life threatening postdose blood pressure (BP) ≥150/90 mm Hg
    • Antihypertensive treatment is not required: Continue treatment at previous dose
    • Antihypertensive treatment is required: Consider dose reduction from 60 mg to 45 mg or from 45 mg to 30 mg
    • Discontinue treatment if BP remains uncontrolled (BP >150/90 mm Hg) despite antihypertensive treatment

Noninfectious pneumonitis (NIP)

  • Grade 2: Withhold copanlisib and treat NIP; resume treatment at 45 mg once NIP recovers to grade 1 or less
  • Grade 2 recurs: Discontinue treatment
  • Grade ≥3: Discontinue treatment

Neutropenia

  • Absolute neutrophil count (ANC) 0.5-1.0 x 103 cells/mm3: Maintain dose; monitor ANC at least weekly
  • ANC <0.5 x 103 cells/mm3: Withhold treatment; monitor ANC at least weekly until ANC ≥0.5 x 103 cells/mm3, then resume treatment at previous dose
  • If ANC ≤0.5 x 103 cells/mm3 recurs, then reduce dose to 45 mg

Severe cutaneous reactions

  • Grade 3: Withhold treatment until toxicity is resolved and reduce dose from 60 mg to 45 mg, or from 45 mg to 30 mg
  • Life-threatening: Discontinue treatment

Thrombocytopenia

  • <25 X 109/L: Withhold treatment; resume when platelet levels return to ≥75 x 109/L; reduce dose from 60 mg to 45 mg, or from 45 mg to 30 mg if recovery occurs within 21 days
  • If recovery does not occur within 21 days, discontinue treatment

Other severe and non-life-threatening toxicities

  • Grade 3: Withhold until toxicity is resolved and reduce dose from 60 mg to 45 mg, or from 45 mg to 30 mg

Hepatic impairment

  • Mild (total bilirubin ≤1x ULN and AST >ULN, or total bilirubin >1-1.5x ULN and any AST): No dosage adjustment necessary
  • Moderate (Child-Pugh B): Reduce dose to 45 mg
  • Severe (Child-Pugh C): Not studied

Marginal Zone Lymphoma (Orphan)

Orphan designation for splenic, nodal, and extranodal subtypes of marginal zone lymphoma

Sponsor

  • Bayer HealthCare Pharmaceuticals, Inc; 100 Bayer Boulevard, PO Box 915; Hanover, New Jersey 07981

Safety and efficacy has not been established

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Interactions

Interaction Checker

and copanlisib

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      Serious - Use Alternative

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            Contraindicated (0)

              Serious - Use Alternative (62)

              • abametapir

                abametapir will increase the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. For 2 weeks after abametapir application, avoid taking drugs that are CYP3A4 substrates. If not feasible, avoid use of abametapir.

              • amobarbital

                amobarbital will decrease the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of copanlisib with strong CYP3A4 inducers.

              • apalutamide

                apalutamide will decrease the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of apalutamide, a strong CYP3A4 inducer, with drugs that are CYP3A4 substrates can result in lower exposure to these medications. Avoid or substitute another drug for these medications when possible. Evaluate for loss of therapeutic effect if medication must be coadministered. Adjust dose according to prescribing information if needed.

              • atazanavir

                atazanavir will increase the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If concomitant use with strong CYP3A inhibitors cannot be avoided, reduce copanlisib dose to 45 mg.

              • bosentan

                bosentan will decrease the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of copanlisib with strong CYP3A4 inducers.

              • butabarbital

                butabarbital will decrease the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of copanlisib with strong CYP3A4 inducers.

              • butalbital

                butalbital will decrease the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of copanlisib with strong CYP3A4 inducers.

              • carbamazepine

                carbamazepine will decrease the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of copanlisib with strong CYP3A4 inducers.

              • chloramphenicol

                chloramphenicol will increase the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              • clarithromycin

                clarithromycin will increase the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If concomitant use with strong CYP3A inhibitors cannot be avoided, reduce copanlisib dose to 45 mg.

              • cobicistat

                cobicistat will increase the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If concomitant use with strong CYP3A inhibitors cannot be avoided, reduce copanlisib dose to 45 mg.

              • conivaptan

                conivaptan will increase the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              • dabrafenib

                dabrafenib will decrease the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of copanlisib with strong CYP3A4 inducers.

              • darunavir

                darunavir will increase the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If concomitant use with strong CYP3A inhibitors cannot be avoided, reduce copanlisib dose to 45 mg.

              • dexamethasone

                dexamethasone will decrease the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of copanlisib with strong CYP3A4 inducers.

              • diltiazem

                diltiazem will increase the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Monitor patients for increased copanlisib effects/toxicities if coadministered with diltiazem. Consider reducing copanlisib dose to 45 mg.

              • efavirenz

                efavirenz will decrease the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of copanlisib with strong CYP3A4 inducers.

              • elvitegravir

                elvitegravir will increase the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If concomitant use with strong CYP3A inhibitors cannot be avoided, reduce copanlisib dose to 45 mg.

              • elvitegravir/cobicistat/emtricitabine/tenofovir DF

                elvitegravir/cobicistat/emtricitabine/tenofovir DF will increase the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If concomitant use with strong CYP3A inhibitors cannot be avoided, reduce copanlisib dose to 45 mg.

              • enzalutamide

                enzalutamide will decrease the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of copanlisib with strong CYP3A4 inducers.

              • eslicarbazepine acetate

                eslicarbazepine acetate will decrease the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of copanlisib with strong CYP3A4 inducers.

              • etravirine

                etravirine will decrease the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of copanlisib with strong CYP3A4 inducers.

              • fexinidazole

                fexinidazole will increase the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Fexinidazole inhibits CYP3A4. Coadministration may increase risk for adverse effects of CYP3A4 substrates.

              • fosamprenavir

                fosamprenavir will increase the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If concomitant use with strong CYP3A inhibitors cannot be avoided, reduce copanlisib dose to 45 mg.

              • fosphenytoin

                fosphenytoin will decrease the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of copanlisib with strong CYP3A4 inducers.

              • grapefruit

                grapefruit will increase the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If concomitant use with strong CYP3A inhibitors cannot be avoided, reduce copanlisib dose to 45 mg.

              • idelalisib

                idelalisib will increase the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If concomitant use with strong CYP3A inhibitors cannot be avoided, reduce copanlisib dose to 45 mg.

              • imatinib

                imatinib will increase the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If concomitant use with strong CYP3A inhibitors cannot be avoided, reduce copanlisib dose to 45 mg.

              • indinavir

                indinavir will increase the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If concomitant use with strong CYP3A inhibitors cannot be avoided, reduce copanlisib dose to 45 mg.

              • isoniazid

                isoniazid will increase the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If concomitant use with strong CYP3A inhibitors cannot be avoided, reduce copanlisib dose to 45 mg.

              • itraconazole

                itraconazole will increase the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If concomitant use with strong CYP3A inhibitors cannot be avoided, reduce copanlisib dose to 45 mg.

              • ivosidenib

                ivosidenib will decrease the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of sensitive CYP3A4 substrates with ivosidenib or replace with alternate therapies. If coadministration is unavoidable, monitor patients for loss of therapeutic effect of these drugs.

              • ketoconazole

                ketoconazole will increase the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If concomitant use with strong CYP3A inhibitors cannot be avoided, reduce copanlisib dose to 45 mg.

              • lonafarnib

                lonafarnib will increase the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration with sensitive CYP3A substrates. If coadministration unavoidable, monitor for adverse reactions and reduce CYP3A substrate dose in accordance with product labeling.

              • lopinavir

                lopinavir will increase the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If concomitant use with strong CYP3A inhibitors cannot be avoided, reduce copanlisib dose to 45 mg.

              • lumacaftor/ivacaftor

                lumacaftor/ivacaftor will decrease the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of copanlisib with strong CYP3A4 inducers.

              • mifepristone

                mifepristone will increase the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              • mitotane

                mitotane will decrease the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of copanlisib with strong CYP3A4 inducers.

              • nafcillin

                nafcillin will decrease the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of copanlisib with strong CYP3A4 inducers.

              • nefazodone

                nefazodone will increase the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If concomitant use with strong CYP3A inhibitors cannot be avoided, reduce copanlisib dose to 45 mg.

              • nelfinavir

                nelfinavir will increase the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If concomitant use with strong CYP3A inhibitors cannot be avoided, reduce copanlisib dose to 45 mg.

              • nevirapine

                nevirapine will decrease the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of copanlisib with strong CYP3A4 inducers.

              • nicardipine

                nicardipine will increase the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If concomitant use with strong CYP3A inhibitors cannot be avoided, reduce copanlisib dose to 45 mg.

              • ombitasvir/paritaprevir/ritonavir & dasabuvir

                ombitasvir/paritaprevir/ritonavir & dasabuvir will increase the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If concomitant use with strong CYP3A inhibitors cannot be avoided, reduce copanlisib dose to 45 mg.

              • oxcarbazepine

                oxcarbazepine will decrease the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of copanlisib with strong CYP3A4 inducers.

              • palifermin

                palifermin increases toxicity of copanlisib by Other (see comment). Avoid or Use Alternate Drug. Comment: Palifermin should not be administered within 24 hr before, during infusion of, or within 24 hr after administration of antineoplastic agents. Coadministration of palifermin within 24 hr of chemotherapy resulted in increased severity and duration of oral mucositis.

              • pentobarbital

                pentobarbital will decrease the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of copanlisib with strong CYP3A4 inducers.

              • phenobarbital

                phenobarbital will decrease the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of copanlisib with strong CYP3A4 inducers.

              • phenytoin

                phenytoin will decrease the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of copanlisib with strong CYP3A4 inducers.

              • posaconazole

                posaconazole will increase the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If concomitant use with strong CYP3A inhibitors cannot be avoided, reduce copanlisib dose to 45 mg.

              • primidone

                primidone will decrease the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of copanlisib with strong CYP3A4 inducers.

              • rifabutin

                rifabutin will decrease the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of copanlisib with strong CYP3A4 inducers.

              • rifampin

                rifampin will decrease the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of copanlisib with strong CYP3A4 inducers.

              • rifapentine

                rifapentine will decrease the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of copanlisib with strong CYP3A4 inducers.

              • ritonavir

                ritonavir will increase the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If concomitant use with strong CYP3A inhibitors cannot be avoided, reduce copanlisib dose to 45 mg.

              • saquinavir

                saquinavir will increase the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If concomitant use with strong CYP3A inhibitors cannot be avoided, reduce copanlisib dose to 45 mg.

              • secobarbital

                secobarbital will decrease the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of copanlisib with strong CYP3A4 inducers.

              • St John's Wort

                St John's Wort will decrease the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of copanlisib with strong CYP3A4 inducers.

              • tipranavir

                tipranavir will increase the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If concomitant use with strong CYP3A inhibitors cannot be avoided, reduce copanlisib dose to 45 mg.

              • tucatinib

                tucatinib will increase the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concomitant use of tucatinib with CYP3A substrates, where minimal concentration changes may lead to serious or life-threatening toxicities. If unavoidable, reduce CYP3A substrate dose according to product labeling.

              • voriconazole

                voriconazole will increase the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If concomitant use with strong CYP3A inhibitors cannot be avoided, reduce copanlisib dose to 45 mg.

              • voxelotor

                voxelotor will increase the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Voxelotor increases systemic exposure of sensitive CYP3A4 substrates. Avoid coadministration with sensitive CYP3A4 substrates with a narrow therapeutic index. Consider dose reduction of the sensitive CYP3A4 substrate(s) if unable to avoid.

              Monitor Closely (17)

              • belzutifan

                belzutifan will decrease the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. If unable to avoid coadministration of belzutifan with sensitive CYP3A4 substrates, consider increasing the sensitive CYP3A4 substrate dose in accordance with its prescribing information.

              • cenobamate

                cenobamate will decrease the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase dose of CYP3A4 substrate, as needed, when coadministered with cenobamate.

              • duvelisib

                duvelisib will increase the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. will increase the level or effect of

              • elagolix

                elagolix will decrease the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Elagolix is a weak-to-moderate CYP3A4 inducer. Monitor CYP3A substrates if coadministered. Consider increasing CYP3A substrate dose if needed.

              • encorafenib

                encorafenib, copanlisib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Encorafenib both inhibits and induces CYP3A4 at clinically relevant plasma concentrations. Coadministration of encorafenib with sensitive CYP3A4 substrates may result in increased toxicity or decreased efficacy of these agents.

              • fedratinib

                fedratinib will increase the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Adjust dose of drugs that are CYP3A4 substrates as necessary.

              • istradefylline

                istradefylline will increase the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Istradefylline 40 mg/day increased peak levels and AUC of CYP3A4 substrates in clinical trials. This effect was not observed with istradefylline 20 mg/day. Consider dose reduction of sensitive CYP3A4 substrates.

              • lorlatinib

                lorlatinib will decrease the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • ofatumumab SC

                ofatumumab SC, copanlisib. Either increases effects of the other by immunosuppressive effects; risk of infection. Use Caution/Monitor. Consider the risk of additive immune system effects when coadministering immunosuppressive therapies with coadministration. When switching from therapies with immune effects, take into account the duration and mechanism of action of these therapies when initiating ofatumumab SC.

              • ribociclib

                ribociclib will increase the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • rucaparib

                rucaparib will increase the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Adjust dosage of CYP3A4 substrates, if clinically indicated.

              • siponimod

                siponimod and copanlisib both increase immunosuppressive effects; risk of infection. Use Caution/Monitor. Caution if coadministered because of additive immunosuppressive effects during such therapy and in the weeks following administration. When switching from drugs with prolonged immune effects, consider the half-life and mode of action of these drugs to avoid unintended additive immunosuppressive effects.

              • stiripentol

                stiripentol, copanlisib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Stiripentol is a CYP3A4 inhibitor and inducer. Monitor CYP3A4 substrates coadministered with stiripentol for increased or decreased effects. CYP3A4 substrates may require dosage adjustment.

              • tazemetostat

                tazemetostat will decrease the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • tecovirimat

                tecovirimat will decrease the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Tecovirimat is a weak CYP3A4 inducer. Monitor sensitive CYP3A4 substrates for effectiveness if coadministered.

              • trastuzumab

                trastuzumab, copanlisib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Use Caution/Monitor. Neutropenia or febrile neutropenia incidence were increased when trastuzumab was coadministered with myelosuppressive chemotherapy. .

              • trastuzumab deruxtecan

                trastuzumab deruxtecan, copanlisib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Use Caution/Monitor. Neutropenia or febrile neutropenia incidence were increased when trastuzumab was coadministered with myelosuppressive chemotherapy. .

              Minor (0)

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                Adverse Effects

                >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

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                Warnings

                Contraindications

                None

                Cautions

                Serious, including fatal, infections may occur; the most common serious infection was pneumonia; before initiating treatment, consider pneumocystis jiroveci pneumonia (PJP) prophylaxis for populations at risk; withhold therapy in patients with suspected PJP infection of any grade; if confirmed, treat infection until resolution, then resume treatment at previous dose with concomitant PJP prophylaxis; 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) 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, 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

                Drug interaction overview

                • Concomitant use of copanlisib with strong CYP3A4 inducers may decrease copanlisib’s AUC and peak plasma concentrations
                • Coadministration with strong CYP3A5 inhibitors may increase the AUC of copanlisib
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                Pregnancy

                Pregnancy

                Based on animal studies and the mechanism of action, copanlisib can cause fetal harm when administered to a pregnant woman

                Advise pregnant women of the potential risk to a fetus

                Conduct pregnancy testing prior to initiation of treatment

                Contraception

                • Advise female patients of reproductive potential to use highly effective contraception during treatment and for at least 1 month after the last dose
                • Advise male patients with female partners of reproductive potential to use highly effective contraception during and for at least 1 month after the last dose

                Lactation

                There are no data on the presence of copanlisib and/or metabolites in human milk, the effects on the breastfed child, or on milk production

                Because of the potential for serious adverse reactions in a breastfed child from copanlisib, advise a lactating woman not to breastfeed during treatment with copanlisib and for at least 1 month after the last dose

                Pregnancy Categories

                A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

                B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

                C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

                D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

                X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

                NA: Information not available.

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                Nutrition

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                Pharmacology

                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%)

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                Administration

                IV Compatibilities

                0.9% NaCl

                IV Preparation

                IV infusion only

                Do not mix or inject copanlisib with other drugs or other diluents

                Reconstitute copanlisib with 4.4 mL of sterile 0.9% NaCl solution for a concentration of 15 mg/mL

                Inspect visually for discoloration and particulate matter; the solution should be colorless to slightly yellowish after reconstitution

                Further dilute the reconstituted solution in 100 mL sterile 0.9% NaCl solution for injection

                Withdraw required amount of the reconstituted solution for the desired dosage (see prescribing information for further information)

                Inject the contents of the syringe into the patient infusion bag of 100 mL sterile 0.9% NaCl solution

                Mix the dose well by inverting

                Use reconstituted and diluted copanlisib immediately or store the reconstituted solution in the vial or diluted solution in the infusion bag at 2-8°C (36-46°F) for up to 24 hours before use

                Avoid exposure of the diluted solution to direct sunlight

                IV Administration

                Allow the product to come to room temperature before use following refrigeration

                Infuse over 1 hr

                Storage

                Unused vials: Refrigerate at 2-8°C (36-46°F)

                Diluted solutions: Refrigerate at 2-8°C (36-46°F) for up to 24 hours before use

                Protect from direct sunlight

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                Images

                No images available for this drug.
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                Patient Handout

                A Patient Handout is not currently available for this monograph.
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                Formulary

                FormularyPatient Discounts

                Adding plans allows you to compare formulary status to other drugs in the same class.

                To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

                Adding plans allows you to:

                • View the formulary and any restrictions for each plan.
                • Manage and view all your plans together – even plans in different states.
                • Compare formulary status to other drugs in the same class.
                • Access your plan list on any device – mobile or desktop.

                The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

                Tier Description
                1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
                2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
                3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
                4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                NC NOT COVERED – Drugs that are not covered by the plan.
                Code Definition
                PA Prior Authorization
                Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
                QL Quantity Limits
                Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
                ST Step Therapy
                Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
                OR Other Restrictions
                Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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                Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.