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Aliqopa

Generic Name: Copanlisib
Class: Antineoplastic Agents
- Kinase Inhibitors
- Phosphatidylinositol-3-Kinase Inhibitors
- Phosphoinositide-3-Kinase Inhibitors
- PI3K Inhibitors
Chemical Name: 2-Amino-N-[7-methoxy-8-[3-(morpholin-4-yl)propoxy]-2,3-dihydroimidazo[1,2-c]quinazolin-5-yl]pyrimidine-5-carboxamide
Molecular Formula: C23H28N8O4C23H28N8O4•2HCl
CAS Number: 1032568-63-0

Medically reviewed by Drugs.com. Last updated on Jan 7, 2019.

Introduction

Antineoplastic agent; an inhibitor of phosphatidylinositol-3-kinase (PI3K) with inhibitory activity mainly against PI3K-α and PI3K-δ isoforms.1 2 3 5 6 7 8

Uses for Aliqopa

Follicular Lymphoma

Treatment of relapsed follicular lymphoma in patients who previously received ≥2 systemic therapies1 2 3 (designated an orphan drug by FDA for this use).4

Current indication based on based on overall response rate; clinical benefit (e.g., improvement in survival) not established.1 2 Continued FDA approval for this indication may be contingent on verification and description of clinical benefit in a confirmatory trial.1

In the pivotal efficacy study (CHRONOS-1), the overall response rate in patients with relapsed follicular lymphoma at the time of data analysis was 59% (with 14% complete responses and 44% partial responses).1 2

Aliqopa Dosage and Administration

General

  • Because copanlisib therapy may increase the risk of developing Pneumocystis jiroveci (formerly Pneumocystis carinii) pneumonia (PCP), consider PCP prophylaxis in patients at risk for PCP prior to initiating copanlisib therapy.1 2 (See Infections under Cautions.)

  • Because of the risk of infusion-related hyperglycemia, achieve optimal glycemic control prior to starting each infusion of copanlisib.1 (See Hyperglycemia under Dosage and Administration.)

  • Because of the risk of infusion-related hypertension, achieve optimal BP control before each copanlisib infusion.1 Monitor BP both before and after infusion.1 (See Hypertension under Dosage and Administration and also under Cautions.)

  • Risk of neutropenia.1 Monitor CBC counts at least weekly during copanlisib therapy.1 (See Hematologic Toxicity under Dosage and Administration.)

Administration

IV Administration

For solution compatibility information, see Compatibility under Stability.

Administer by IV infusion.1

Copanlisib hydrochloride lyophilized solid for injection must be reconstituted and diluted prior to administration.1

Do not infuse simultaneously through the same IV line with other drugs.1

Reconstitution

Reconstitute vial containing 60 mg of copanlisib as a lyophilized solid with 4.4 mL of 0.9% sodium chloride injection to provide a solution containing 15 mg/mL.1 No other diluent should be used.1 Gently shake vial for 30 seconds, then allow solution to stand for 1 minute to allow bubbles to rise to surface.1 If undissolved substance remains in the vial, gently shake vial for another 30 seconds, then allow solution to stand for another minute to settle.1

Inspect reconstituted solution visually for particulate matter and discoloration prior to dilution and administration.1 Reconstituted solution should be colorless to slightly yellow.1 Once free of visible particles, may withdraw reconstituted solution for further dilution.1

Dilution

Dilute appropriate dose in 100 mL of 0.9% sodium chloride injection.1 For 60-, 45-, or 30-mg doses, withdraw 4, 3, or 2 mL of reconstituted solution with a sterile syringe, respectively, and add to the container.1 Mix the diluted solution by gentle inversion.1 Discard any unused reconstituted or diluted solution appropriately.1

Rate of Administration

Administer over 60 minutes.1

Dosage

Dosage of copanlisib hydrochloride expressed in terms of copanlisib.1

Adults

Follicular Lymphoma
Relapsed Follicular Lymphoma Following Failure of ≥2 Prior Systemic Therapies
IV

60 mg on days 1, 8, and 15 of each 28-day cycle on an intermittent schedule (3 weeks on and 1 week off).1 Continue therapy until disease progression or unacceptable toxicity occurs.1

Dosage Modification for Toxicity

May need to interrupt therapy, reduce dosage, and/or permanently discontinue copanlisib if toxicity occurs.1 If therapy is interrupted for toxicity, ≥7 days must elapse between 2 consecutive infusions.1 Discontinue therapy if life-threatening, copanlisib-related toxicity occurs.1

Infections

If grade 3 or 4 infection occurs, withhold copanlisib until infection resolves, then resume copanlisib at previous dosage.1 (See Infections under Cautions.)

If any grade of Pneumocystis jiroveci (formerly Pneumocystis carinii) pneumonia (PCP) is suspected, withhold copanlisib.1 If PCP infection is confirmed, treat the infection.1 When the pneumonia resolves, resume therapy at previous dosage with concomitant PCP prophylaxis.1

Hyperglycemia

If fasting blood glucose concentrations ≥160 mg/dL or random/nonfasting blood glucose concentrations ≥200 mg/dL occur prior to copanlisib infusion, withhold copanlisib.1 When fasting blood glucose concentrations are ≤160 mg/dL, or random/nonfasting blood glucose concentrations are ≤200 mg/dL, resume therapy.1

If predose or postdose blood glucose concentrations ≥500 mg/dL occur for the first time, withhold copanlisib.1 When fasting blood glucose concentration is ≤160 mg/dL, or random/nonfasting blood glucose concentration is ≤200 mg/dL, resume copanlisib therapy at a reduced dosage of 45 mg and maintain.1 If predose or postdose blood glucose concentrations ≥500 mg/dL recur, withhold therapy.1 When fasting blood glucose concentrations are ≤160 mg/dL, or random/nonfasting blood glucose concentrations are ≤200 mg/dL, resume therapy at a reduced dosage of 30 mg and maintain.1 If predose or postdose blood glucose concentrations ≥500 mg/dL persist at the reduced dosage of 30 mg, permanently discontinue copanlisib.1 (See Hyperglycemia under Cautions.)

Hypertension

If both SBP/DBP ≥150/90 mm Hg prior to copanlisib infusion, withhold copanlisib.1 When both systolic/diastolic BP are <150/90 mm Hg for 2 consecutive BP measurements taken at least 15 minutes apart, resume therapy.1

If non-life-threatening SBP/DBP ≥150/90 mm Hg (both systolic and diastolic) occurs after copanlisib infusion and antihypertensive therapy is not required, continue copanlisib at previous dosage.1 If antihypertensive therapy is necessary, consider reduction in dosage (i.e., reduce dosage of 60 mg to 45 mg; reduce dosage of 45 mg to 30 mg).1 If both SBP/DBP remain ≥150/90 mm Hg despite antihypertensive therapy, permanently discontinue copanlisib.1

If life-threatening hypertension occurs after infusion of copanlisib, permanently discontinue the drug.1 (See Hypertension under Cautions.)

Noninfectious Pneumonitis

If grade 2 noninfectious pneumonitis occurs, withhold copanlisib.1 When symptoms resolve to grade 1 or less, may resume therapy at a reduced dosage of 45 mg.1 If grade 2 noninfectious pneumonitis recurs, permanently discontinue copanlisib.1

If grade 3 or greater noninfectious pneumonitis occurs, permanently discontinue copanlisib.1 (See Noninfectious Pneumonitis under Cautions.)

Hematologic Toxicity

Neutropenia and thrombocytopenia have occurred.1

If ANC is 500 to 1000/mm3, continue copanlisib at the same dosage; monitor ANC at least weekly.1 (See Neutropenia under Cautions.)

If ANC is <500/mm3, withhold copanlisib; monitor ANC at least weekly.1 When ANC is ≥500/mm3, resume therapy at previous dosage.1 If ANC <500/mm3 recurs, reduce dosage to 45 mg.1 (See Neutropenia under Cautions.)

If platelet count is <25,000/mm3, withhold copanlisib until platelet count is ≥75,000/mm3.1 If platelet recovery occurs within 21 days and previous dosage was 60 mg, reduce dosage to 45 mg; if previous dosage was 45 mg, reduce dosage to 30 mg.1 If platelet recovery does not occur within 21 days, permanently discontinue copanlisib.1

Dermatologic Toxicity

If grade 3 severe dermatologic reactions occur, withhold copanlisib; when toxicity resolves, resume therapy at a reduced dosage.1 If previous dosage was 60 mg, reduce dosage to 45 mg; if previous dosage was 45 mg, reduce dosage to 30 mg.1

If life-threatening dermatologic toxicity occurs, permanently discontinue copanlisib.1 (See Dermatologic Effects under Cautions.)

Other Toxicities

If grade 3 severe (but not life-threatening) toxicity occurs, withhold copanlisib; when toxicity resolves, resume copanlisib therapy at a reduced dosage (i.e., reduce dosage of 60 mg to 45 mg; reduce dosage of 45 mg to 30 mg).1

Concomitant Use with Drugs and Foods Affecting Microsomal Enzymes

Concomitant use of copanlisib and drugs or foods that are potent inhibitors of CYP3A may result in increased copanlisib exposure and increase the risk of toxicity.1 If concomitant use of potent CYP3A inhibitors cannot be avoided, reduce copanlisib dosage to 45 mg.1 (See Interactions.)

Special Populations

Hepatic Impairment

No specific dosage recommendations at this time.1 (See Hepatic Impairment under Cautions.)

Renal Impairment

No specific dosage recommendations at this time.1 (See Renal Impairment under Cautions.)

Geriatric Patients

Dosage adjustment not necessary in patients ≥65 years of age; nearly half of patients in pivotal efficacy study were geriatric.1 (See Geriatric Use under Cautions.)

Cautions for Aliqopa

Contraindications

  • No known contraindications.1

Warnings/Precautions

Warnings

Infections

Serious, including fatal, infections reported in 19% of patients receiving copanlisib therapy in clinical trials.1 2 Pneumonia was the most frequently reported serious infection.1 2

Serious Pneumocystis jiroveci (formerly Pneumocystis carinii) pneumonia (PCP) reported in 0.6% of patients receiving copanlisib monotherapy in clinical trials.1 2 Prior to initiating copanlisib therapy, consider PCP prophylaxis for populations at risk for PCP.1 If PCP of any grade is suspected, withhold copanlisib.1 If PCP is confirmed, treat the infection; when the infection resolves, resume copanlisib at previous dosage with concomitant PCP prophylaxis.1

Monitor for signs and symptoms of infection during copanlisib therapy.1 If grade 3 or greater infection occurs, withhold copanlisib.1 (See Infections under Dosage and Administration.)

Hyperglycemia

Risk of infusion-related hyperglycemia.1 2 Grade 3 or 4 hyperglycemia (blood glucose concentrations ≥250 mg/dL) reported in 41% of patients in clinical studies.1 Elevated blood glucose concentrations usually peaked 5–8 hours post-infusion, and then gradually declined to baseline within 24 hours in most patients.1 2 Blood glucose concentrations remained elevated in 17.7% of patients 1 day after copanlisib infusion.1 In clinical studies, an increase in glycosylated hemoglobin (hemoglobin A1c; HbA1c) concentration exceeding 6.5% occurred at the end of treatment in 10% of patients with a baseline HbA1c of 5.7% or less.1

In patients with diabetes mellitus, achieve adequate glycemic control prior to initiating copanlisib therapy; closely monitor such patients during therapy.1

Prior to each copanlisib infusion, achieve optimal glycemic control.1 If hyperglycemia occurs, temporary interruption of copanlisib therapy and/or dosage reduction or discontinuance of therapy may be necessary depending on the severity and persistence of hyperglycemia.1 (See Hyperglycemia under Dosage and Administration and also see Advice to Patients.)

Hypertension

Risk of infusion-related hypertension.1 Grade 3 hypertension (SBP ≥160 mm Hg or DBP ≥100 mm Hg) reported in 26% of patients receiving copanlisib monotherapy in clinical trials; serious hypertensive events reported in 0.9% of these patients.1 BP peaked approximately 2 hours after infusion, and then gradually decreased; BP remained elevated for 6–8 hours after initiating the infusion.1

Achieve optimal BP control prior to each copanlisib infusion.1 Monitor BP before and following each infusion.1 May need to interrupt therapy, reduce dosage, and/or permanently discontinue copanlisib depending on severity and persistence of hypertension.1 (See Hypertension under Dosage and Administration.)

Noninfectious Pneumonitis

Noninfectious pneumonitis reported.1

Evaluate patients for possible pneumonitis if pulmonary manifestations (e.g., cough, dyspnea, hypoxia, interstitial infiltrates on radiologic exam) occur.1 If pneumonitis is suspected, withhold therapy.1

Treatment for copanlisib-induced pneumonitis has included discontinuance of copanlisib and administration of systemic corticosteroids.1 May also need to reduce dosage and/or permanently discontinue the drug depending on severity and persistence of pneumonitis.1 (See Noninfectious Pneumonitis under Dosage and Administration.)

Neutropenia

Severe (grade 3 or 4) neutropenia reported.1

Monitor CBC counts at least weekly during therapy.1 May need to interrupt therapy, reduce dosage, and/or permanently discontinue copanlisib depending on severity and persistence of neutropenia.1 (See Hematologic Toxicity under Dosage and Administration.)

Dermatologic Effects

Severe dermatologic reactions, including exfoliative dermatitis, pruritus, and rash (e.g., exfoliative rash, maculopapular rash) reported.1

May need to interrupt therapy, reduce dosage, and/or permanently discontinue copanlisib depending on severity and persistence of severe dermatologic reaction.1 (See Dermatologic Toxicity under Dosage and Administration.)

Fetal/Neonatal Morbidity and Mortality

Based on its mechanism of action and animal findings, copanlisib may cause fetal harm.1 Embryofetal toxicity and teratogenicity demonstrated in animals.1 (See Distribution under Pharmacokinetics.)

Perform a pregnancy test prior to initiation of copanlisib therapy in women of childbearing potential.1 Avoid pregnancy during therapy and for ≥1 month after drug discontinuance.1 Advise women of childbearing potential and men who are partners of such women to use highly effective contraception (i.e., contraception with a failure rate of <1% per year) while receiving the drug and for ≥1 month after discontinuance of therapy.1 If used during pregnancy or if patient becomes pregnant, apprise of potential fetal hazard.1 (See Advice to Patients.)

Specific Populations

Pregnancy

Based on its mechanism of action and animal findings, may cause fetal harm.1 (See Fetal/Neonatal Morbidity and Mortality under Cautions.)

Lactation

Distributed into milk in rats; not known whether drug and/or metabolites distribute into human milk or if drug has any effect on milk production or the nursing infant.1

Because of the potential for serious adverse reactions to copanlisib in nursing infants, women should not breast-feed during therapy and for ≥1 month following drug discontinuance.1 (See Distribution under Pharmacokinetics.)

Pediatric Use

Safety and efficacy not established in pediatric patients.1

Geriatric Use

In clinical studies evaluating copanlisib in patients with follicular lymphoma and other hematologic malignancies, 48% of patients were ≥65 years of age and 16% were ≥75 years of age.1 No clinically important differences in efficacy in geriatric patients (≥65 years of age) compared with younger adults.1

Higher incidences of serious adverse reactions and discontinuance of copanlisib due to adverse reactions observed in patients ≥65 years of age compared with younger adults.1 (See Special Populations under Pharmacokinetics.)

Hepatic Impairment

Pharmacokinetics not affected by mild hepatic impairment (bilirubin concentration not greater than ULN with AST concentration greater than ULN, or bilirubin concentration <1–1.5 times ULN with any AST concentration).1 Data are not available for patients with moderate or severe hepatic impairment.1 (See Special Populations under Dosage and Administration.)

Renal Impairment

Pharmacokinetics not affected by mild or moderate renal impairment (Clcr ≥30 mL/minute).1 Not studied in patients with severe renal impairment (Clcr <30 mL/minute) or in patients with end-stage renal disease, including those undergoing dialysis.1 (See Special Populations under Dosage and Administration.)

Common Adverse Effects

Hyperglycemia,1 2 3 6 diarrhea,1 2 3 decreased general strength and energy,1 2 3 hypertension,1 2 3 6 leukopenia,1 neutropenia,1 2 nausea,1 2 3 6 lower respiratory tract infections,1 thrombocytopenia.1 2

Interactions for Aliqopa

Metabolized principally by CYP3A and, to a lesser extent (<10%), by CYP1A1.1

Not expected to inhibit CYP isoenzymes 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, or 3A4, or UGT or dihydropyrimidine dehydrogenase (DPD).1 Not expected to inhibit efflux transporter P-glycoprotein (P-gp), breast cancer resistance protein (BCRP), multi-drug resistance-associated protein (MRP2), bile salt export pump (BSEP), organic anion transport protein (OATP) 1B1, OATP1B3, renal organic anion transporter (OAT) 1, OAT3, organic cation transporter (OCT) 1, OCT2, and multidrug and toxin extrusion protein 1 (MATE1).1 Inhibits MATE2-K.1

Substrate of P-gp and BCRP; not a substrate of OATP1B1, OATP1B3, OAT1, OAT3, OCT 1, OCT2, OCT3, MATE1 or MATE2-K.1

Does not induce CYP isoenzymes 1A2, 2B6, or 3A.1

Drugs Affecting Hepatic Microsomal Enzymes

Potent inhibitors of CYP3A: Potential pharmacokinetic interaction (increased systemic exposure to copanlisib and increased risk of toxicity).1 If concomitant use cannot be avoided, reduce copanlisib dosage.1 (See Concomitant Use with Drugs or Foods Affecting Microsomal Enzymes under Dosage and Administration.)

Potent inducers of CYP3A: Potential pharmacokinetic interaction (decreased systemic exposure to copanlisib).1 Avoid concomitant use.1

Drugs Affecting the P-glycoprotein Transport System

P-gp inhibitors: Potential pharmacokinetic interaction (increased systemic exposure to copanlisib).1

P-gp inducers Potential pharmacokinetic interaction (decreased systemic exposure to copanlisib).1

Drugs Affected by Other Membrane Transporters

MATE2-K substrates; Based on pharmacokinetics of copanlisib, MATE2-K inhibition may occur following infusion of the drug at the recommended dosage.1 The clinical importance of this potential inhibition not known.1

Specific Drugs and Foods

Drug or food

Interaction

Comments

Anticonvulsants (carbamazepine, phenytoin)

Possible decreased AUC and peak plasma concentrations of copanlisib1

Avoid concomitant use1

Antifungals, azoles (e.g., itraconazole, ketoconazole, posaconazole, voriconazole)

Possible increased systemic exposure to copanlisib1

Itraconazole: Increased AUC of copanlisib; peak plasma concentrations of copanlisib not affected1

If concomitant use cannot be avoided, decrease copanlisib dosage to 45 mg1

Boceprevir

Possible increased systemic exposure to copanlisib1

If concomitant use cannot be avoided, decrease copanlisib dosage to 45 mg1

Clarithromycin

Possible increased systemic exposure to copanlisib1

If concomitant use cannot be avoided, decrease copanlisib dosage to 45 mg1

Cobicistat

Possible increased systemic exposure to copanlisib1

If concomitant use cannot be avoided, decrease copanlisib dosage to 45 mg1

Conivaptan

Possible increased systemic exposure to copanlisib1

If concomitant use cannot be avoided, decrease copanlisib dosage to 45 mg1

Diltiazem

Possible increased systemic exposure to copanlisib1

If concomitant use cannot be avoided, decrease copanlisib dosage to 45 mg1

Elvitegravir (with ritonavir)

Possible increased systemic exposure to copanlisib1 9 10

If concomitant use cannot be avoided, decrease copanlisib dosage to 45 mg1

Enzalutamide

Possible decreased AUC and peak plasma concentrations of copanlisib1

Avoid concomitant use1

Grapefruit juice

Possible increased systemic exposure to copanlisib1

Avoid concomitant use1

HIV protease inhibitors (PIs; e.g., nelfinavir, ritonavir, and fixed combinations of indinavir, lopinavir, saquinavir, and tipranavir with ritonavir; saquinavir, tipranavir)

Possible increased systemic exposure to copanlisib1

If concomitant use cannot be avoided, decrease copanlisib dosage to 45 mg1

Idelalisib

Possible increased systemic exposure to copanlisib1

Avoid concomitant use; if concomitant use cannot be avoided, decrease copanlisib dosage to 45 mg1

Mitotane

Possible decreased AUC and peak plasma concentrations of copanlisib1

Avoid concomitant use1

Nefazodone

Possible increased systemic exposure to copanlisib1

If concomitant use cannot be avoided, decrease copanlisib dosage to 45 mg1

Paritaprevir

Available in fixed combination with dasabuvir and/or ombitasvir and ritonavir: Possible increased systemic exposure to copanlisib1

If concomitant use cannot be avoided, decrease copanlisib dosage to 45 mg1

Rifampin

Decreased AUC and peak plasma concentrations of copanlisib1

Avoid concomitant use1

St. John's wort (Hypericum perforatum)

Possible decreased AUC and peak plasma concentrations of copanlisib1

Avoid concomitant use1

Aliqopa Pharmacokinetics

Absorption

Plasma Concentrations

AUC and peak plasma concentration increase in a dose-proportional manner over a dosage range of 5–93 mg.1

Distribution

Extent

Not known whether copanlisib and/or metabolites distribute into human milk.1 In lactating rats, approximately 2% of the radioactivity from a radiolabeled dose of copanlisib was secreted into milk; the milk to plasma ratio of radioactivity was 25-fold.1

Copanlisib and metabolites cross the placenta.1 Following administration of radiolabeled drug to pregnant animals, approximately 1.5% of the radioactivity reached the fetal compartment.1

Plasma Protein Binding

84.2% (mainly to albumin).1

Elimination

Metabolism

Principally metabolized (approximately 90%) by CYP3A and to a lesser extent (<10%) by CYP1A1.1

Principal active metabolite is —1, which accounts for 5% of total radioactivity AUC and has comparable pharmacologic activity (i.e., PI3K-α and PI3K-δ inhibition) as the parent drug.1

Elimination Route

Eliminated in feces (approximately 64% [about 30% as unchanged drug]) and urine (approximately 22% [about 15% as unchanged drug]).1 Metabolites from CYP-mediated metabolism accounted for 41% of administered dose.1

Half-life

Mean terminal half-life: 39.1 hours (range: 14.6–82.4 hours).1

Special Populations

In a pharmacokinetic population analysis, age (20–90 years), gender, race, smoking status, body weight, mild hepatic impairment, and mild or moderate renal impairment did not have clinically important effects on copanlisib pharmacokinetics.1

Not studied in patients with moderate or severe hepatic impairment, severe renal impairment, or end-stage renal disease (with or without dialysis).1

Stability

Storage

Parenteral

Solid for Injection

Store unopened vials at 2–8°C.1

Following reconstitution or dilution, use solution immediately or store at 2–8°C in the original vial or infusion bag for ≤24 hours.1

Following refrigeration of the diluted infusion solution, allow solution to adapt to room temperature prior to administration.1 Protect diluted solution from direct sunlight.1

Compatibility

For information on systemic interactions resulting from concomitant use, see Interactions.

Parenteral

Solution Compatibility

Compatible

Sodium chloride 0.9%1

Actions

  • Inhibits phosphatidylinositol-3-kinase (PI3K).1 2 3 5 6 7 8 Phosphatidylinositol-3-kinases are lipid kinases consisting of a catalytic subunit that exists in 4 different isoforms (α, β, γ, δ).5 7 Copanlisib is a pan-class inhibitor of PI3K that is predominantly active against the PI3K-α and PI3K-δ isoforms.1 2 3 5 6 7 8

  • The PI3K-α and PI3K-δ isoforms are expressed in malignant B cells.5 7

  • Induces apoptosis and inhibits proliferation of primary malignant B-cell lines.1 6

  • Inhibits several important cell signaling pathways, including B-cell receptor (BCR) signaling, CXCR12-mediated chemotaxis of malignant B cells, and NFκB signaling in lymphoma cell lines.1 7

Advice to Patients

  • Importance of instructing patients to read the manufacturer's patient information.1

  • Risk of serious infections such as pneumonia.1 Importance of immediately reporting fever or any other signs of infection.1

  • Risk of infusion-related hyperglycemia.1 Importance of reporting signs or symptoms of hyperglycemia (e.g., pronounced hunger, excessive thirst, frequent urination, headaches).1 Blood glucose concentrations should be well controlled prior to infusions of copanlisib.1

  • Risk of infusion-related hypertension.1 Importance of informing clinician if any symptoms of hypertension (e.g., dizziness, fainting, headache, pounding heart) occur during therapy.1 Importance of advising patients that BP should be normal or well controlled prior to copanlisib infusion.1

  • Risk of noninfectious pneumonitis.1 Importance of informing clinician if new or worsening respiratory symptoms (e.g., cough, dyspnea) occur.1

  • Risk of neutropenia.1 Importance of periodically monitoring CBC during copanlisib therapy.1 Importance of immediately informing clinician if fever or other signs of infection occur.1

  • Risk of severe dermatologic reactions.1 Importance of immediately informing clinician if dermatologic reactions (e.g., rash, redness, swelling, itching or peeling skin) occur during copanlisib therapy.1

  • Risk of fetal harm.1 Necessity of advising women of childbearing potential to avoid pregnancy and to use effective contraceptive methods while receiving copanlisib and for ≥1 month following discontinuance of therapy.1 Importance of women informing clinicians immediately if they become pregnant during therapy or think they may be pregnant.1 If pregnancy occurs, advise pregnant women of potential risk to the fetus.1

  • Importance of advising women to avoid breast-feeding while receiving copanlisib and for ≥1 month after discontinuance of therapy.1

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs and dietary or herbal supplements, as well as any concomitant illnesses.1

  • Importance of informing patients of other important precautionary information.1 (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

Copanlisib Hydrochloride

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Parenteral

For injection, for IV infusion only

60 mg (of copanlisib)

Aliqopa

Bayer

AHFS DI Essentials™. © Copyright 2019, Selected Revisions January 7, 2019. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

References

1. Bayer HealthCare Pharmaceuticals, Inc. Aliqopa (copanlisib) for injection prescribing information. Whippany, NJ; 2017 Sep.

2. Dreyling M, Santoro A, Mollica L et al. Phosphatidylinositol 3-kinase inhibition by copanlisib in relapsed or refractory indolent lymphoma. J Clin Oncol. 2017; 35:3898-905.

3. Dreyling M, Morschhauser F, Bouabdallah K et al. Phase II study of copanlisib, a PI3K inhibitor, in relapsed or refractory, indolent or aggressive lymphoma. Ann Oncol. 2017; 28:2169-78.

4. US Food and Drug Administration. Search orphan drug designations and approvals. From FDA website. Accessed 2017 Dec 29. http://www.accessdata.fda.gov/scripts/opdlisting/oopd/index.cfm

5. Lampson BL, Brown JR. PI3Kδ-Selective and PI3Kα/δ-combinatorial inhibitors in clinical development for B-cell non-Hodgkin lymphoma. Expert Opin Investig Drugs. 2017; 26:126779.

6. Patnaik A, Appleman LJ, Tolcher AW et al. First-in-human phase I study of copanlisib (BAY 80-6946), an intravenous pan-class I phosphatidylinositol 3-kinase inhibitor, in patients with advanced solid tumors and non-Hodgkin’s lymphomas. Ann Oncol. 2016; 27:1928-40.

7. US Food and Drug Administration. Center for Drug Evaluation and Research. Application number 209936Orig1s000: Multi-discipline review. From FDA website. https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209936Orig1s000MultidisciplineR.pdf

8. Cho D. Exploring the pathway: despite lukewarm clinical benefit of PI3K inhibitors, optimism remains regarding biomarkers and combination therapy. American Society of Clinical Oncology (ASCO) Daily News. 2015 May 21. https://am.asco.org/exploring-pathway-despite-lukewarm-clinical-benefit-pi3k-inhibitors-optimism-remains-regarding

9. Gilead Sciences, Inc. Stribild (elvitegravir, cobicistat, emtricitabine, tenofovir disoproxil fumarate) film-coated tablets prescribing information. Foster City, CA; 2017 Aug.

10. US Food and Drug Administration. Drug development and drug interactions: table of substrates, inhibitors and inducers. From FDA website. Accessed 2018 Jul 4. https://www.fda.gov/drugs/developmentapprovalprocess/developmentresources/druginteractionslabeling/ucm093664.htm

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