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Drug Formulary information is intended for use by healthcare professionals. It is not intended to be medical advice. Some of the information, including information about funding for cancer drugs, does not apply to all patients. Cancer treatment plans are unique to each patient. If you are a patient, please speak with your healthcare team to understand how this information applies to you.


( all-dess-LOO-kin )
New Drug Funding Program
  • Aldesleukin (interleukin-2) - In-Transit Metastases from Melanoma
Other Name(s): Proleukin® (interleukin-2)
Appearance: Clear/colorless to slightly yellow solution mixed into larger bags of fluids
A - Drug Name


SYNONYM(S):   interleukin-2; IL-2; lymphocyte mitogenic factor; T-cell growth factor; thymocyte stimulating factor

COMMON TRADE NAME(S):   Proleukin® (interleukin-2)

B - Mechanism of Action and Pharmacokinetics

Aldesleukin, a recombinant interleukin-2, has multiple immunologic effects, including activation of cellular immunity with lymphocytosis, eosinophilia, thrombocytopenia and production of lymphokines including TNF, IL-1 and gamma-interferon. Tumour growth inhibition has been reported in in vivo studies. Objective responses are seen in ± 16% of patients but no overall survival benefit in controlled studies has been demonstrated.

Oral: no

Pharmacokinetics appear to be dose proportional. Uptake into lung, liver, spleen and kidney is rapid.

Cross blood brain barrier? No information found
PPB No information found

Aldesleukin is rapidly metabolized to its composite amino acids in the proximal tubules of the kidney.

Active metabolites Trace
Inactive metabolites Yes (to its composite amino acids)

2- compartmental disposition, cleared as inactive metabolites by glomerular filtration and peritubular extraction

Clearance 268mL/minute
Half-life 13-85 minutes
Urine 80% via renal tubular and glomerular filtration
C - Indications and Status
Health Canada Approvals:

  • Carefully selected adults with metastatic renal cell carcinoma
  • Carefully selected adults with metastatic malignant melanoma

D - Adverse Effects

Emetogenic Potential:  

Minimal (Intralesional)
Low (IV doses ≤ 12 MU/m2)
Moderate (IV doses >12-15 MU/m2)

Extravasation Potential:   None

Cardiovascular Arterial thromboembolism (rare) E
Cardiotoxicity (<1%) E
Venous thromboembolism (rare) E
Ventricular arrhythmia (12%) (supraventricular) I
Dermatological Other (persistent vitiligo; rare) E
Rash (42%) (may be exfoliative) I  E
Gastrointestinal Abdominal pain (11%) E
Anorexia (20%) E
Diarrhea (67%) E
GI perforation (or obstruction, +/- bleeding; rare) E
Mucositis (22%) E
Nausea, vomiting (50%) I  E
General Fatigue (27%) E
Flu-like symptoms (52%) I
Hyperthermia (1%) (malignant hyper or hypothermia) E
Hematological Disseminated intravascular coagulation (1%) I
Myelosuppression ± infection, bleeding (37%) (severe 1%) E
Hepatobiliary ↑ LFTs (40%) (may be severe) E
Pancreatitis (rare) E
Hypersensitivity Drug reaction (rare) E
Immune Other (risk of rejection in allograft recipients, exacerbation of autoimmune diseases) E  D
Infection Infection (13%) (may be severe, including atypical) E
Metabolic / Endocrine Abnormal electrolyte(s) (12%) (decreased Ca, Mg) E
Acidosis (12%) I  E
Musculoskeletal Rhabdomyolysis (especially with interferon; rare) E
Nervous System Confusion (34%) (includes somnolence) E
Depression (4%) (may be severe) E  D
Dizziness (11%) E
Leukoencephalopathy (rare) E
Neuropathy (6%; optic neuritis, demyelination-rare) E
Seizure (<1%) E
Ophthalmic Conjunctivitis (2%) E
Eye disorders (1%) E
Renal Creatinine increased (33%) (may be severe) E
Tumor lysis syndrome (with chemotherapy) E
Respiratory Acute respiratory distress syndrome (ARDS) (3%) E
Dyspnea (43%) E
Vascular Capillary leak syndrome (71%) I  E
Vasculitis (cutaneous; cerebral- rare) E

* "Incidence" may refer to an absolute value or the higher value from a reported range.
"Rare" may refer to events with < 1% incidence, reported in post-marketing, phase 1 studies,
isolated data or anecdotal reports.

** I = immediate (onset in hours to days)     E = early (days to weeks)
D = delayed (weeks to months)      L = late (months to years)

Most adverse reactions usually reverse or improve within 2-3 days of discontinuing therapy, due to aldesleukin’s short half-life, but drug-related deaths occur in 2-4% of patients treated with aldesleukin.

The major dose-limiting side effect of aldesleukin is capillary leak syndrome. Aldesleukin administration induces decreased vascular tone and increased vascular permeability leading to hypotension, reduced organ perfusion and function (renal, cardiac, hepatic, etc.), ascites, effusions, cardiac arrhythmias/ischemia and respiratory insufficiency. The management of capillary leak syndrome involves careful monitoring of fluid and organ perfusion. Administration of intravenous dopamine or phenylephrine to increase blood pressure may help maintain organ perfusion, particularly renal perfusion and thereby preserve urine output. Administration of subsequent doses of aldesleukin should be delayed until recovery of organ perfusion is observed.

Renal dysfunction is reversible and also usually secondary to capillary leak syndrome. It is also correlated with the dose, duration of treatment and the patient’s baseline renal function. The administration of indomethacin for flu-like syndrome may potentiate renal dysfunction by decreasing intrarenal prostaglandins.

A flu-like syndrome (fever, rigors and chills) develops in most patients receiving aldesleukin. Treatment with acetaminophen or a NSAID (e.g. ibuprofen, indomethacin) may minimize the risk, but renal function should be monitored carefully. In clinical trials, meperidine was administered to control the rigors associated with fever.

The clinical significance of developing non-neutralizing anti-interleukin-2 antibodies to aldesleukin is unknown. The incidence of antibodies formation is less than 1%. Exacerbation of autoimmune disorders such as Crohns, myasthenia, vasculitis, hypo or hyperthyroidism and diabetes mellitus may also occur.

Hypersensitivity has been described and may be exacerbated when aldesleukin is administered with other drugs; delayed reactions may occur with contrast media.

CNS toxicity is dose-related and generally reversible, but it may be associated with demyelination and may be irreversible in some patients.

E - Dosing

Refer to protocol by which patient is being treated.

Screen for hepatitis B virus in all cancer patients starting systemic treatment. Refer to the hepatitis B virus screening and management guideline.

Patients must be managed as an inpatient in a tertiary care setting with full ICU facilities. Consider the following pre-medications (generally discontinued 12 hours after the last dose of aldesleukin):

  • prophylactic antibiotics in patients with indwelling catheters
  • Antipyretics
  • H2 antagonists
  • Start meperidine and antidiarrheals early at the onset of symptoms.

Note: 1 MU = 1 million units = 1 million IU (international units) = 0.061 mg


Optimal dosage and regimen for aldesleukin have not been established, but the following regimen has been approved by Health Canada.

Intravenous: 600,000 IU/kg (by a 15-minute infusion q8h; maximum 14 doses x 2)












































   (X refers to a single dose)

The course may be repeated 7 weeks after hospital discharge, if tolerable and there is evidence of anti-tumour response.


Dosage with Toxicity:

Aldesleukin should be held for toxicity rather than reducing the dose to be given. Consult the product monograph for detailed management recommendations.

Dose interruption:

Body system



May Restart after Recovery

Discontinue permanently



Atrial fibrillation, SVT, bradycardia



Hypotension – pressors needed



EKG ischemia or myocarditis



Sustained VT, incontrollable arrhythmia



Angina, AMI, tamponade




O2 saturation < 94% on room air or

< 90% with 2 liters O2



Intubation for > 72hrs




Moderate-severe confusion, agitation, lethargy or somnolence



Coma, psychosis > 48 hrs



Uncontrollable seizures




Grade 4, unstable




Serum creatinine > 400 µmol/L

Oliguria -  < 10 mL/hour for 16-24 hours with ↑ creatinine



Dialysis required ≥ 72hrs




Hepatic failure**




Bullous dermatitis




Ischemia, perforation



Bleed not requiring surgery



Bleed requiring surgery



**Abandon course. Do not start new course for at least 7 weeks after recovery.

Dosage in myelosuppression: No adjustment required

Dosage with Hepatic Impairment:

Hold until recovery if any signs of hepatic failure are present. See table above.

Dosage with Renal Impairment:

Do not start treatment if creatinine > 130 µmol/L. See table above.

Dosage in the elderly:

Limited data in elderly patients.  Monitor renal function closely as the elderly may have decreased renal function.


Safety and effectiveness in children under 18 years of age have not been established.

F - Administration Guidelines
  • Each vial (1.3 mg) should be reconstituted with 1.2 mL of SWI.
  • During reconstitution, SWI USP should be directed at the side of the vial and the contents gently swirled to avoid excess foaming. Do not shake.
  • Addition of BSWI or NS may promote aggregation and these solutions should not be used
  • For IV administration, dilute further in 50 mL bag of D5W; infuse over 15 minutes
  • Final concentration of drug should be 30 - 70µg/mL
  • Drug delivery is more consistent when diluted in PVC container rather than non-PVC container
  • In-line filter should not be used when administering aldesleukin
  • Keep refrigerated; do not freeze. Avoid exposure to heat and light.
G - Special Precautions

  • known allergic reaction to aldesleukin, interleukin-2 or any components of the product
  • abnormal thallium stress test
  • abnormal pulmonary function tests
  • organ allografts
  • significant cardiac, pulmonary, renal, hepatic or CNS impairment
  • concomitant use of cisplatin, vinblastine and dacarbazine as fatal tumour lysis syndrome has been reported

Other Warnings/Precautions:

  • use with extreme caution in patients with known cardiac, pulmonary or seizure disorders (even with normal thallium and pulmonary function tests)
  • use with extreme caution in patients with large fluid requirements (e.g., hypercalcemia)
  • use with caution in patients with inflammatory or autoimmune disorders
  • use with caution in combination with antihypertensives and psychotropic drugs as well as hepatotoxic, cardiotoxic or nephrotoxic drugs

Other Drug Properties:

  • Carcinogenicity: Unknown

Pregnancy and Lactation:
  • Embryotoxicity: Probable

    Aldesleukin is not recommended for use in pregnancy.  Adequate contraception should be used by patients and their partners during treatment, and for at least 6 months after the last dose (general recommendation).

  • Excretion into breast milk: Unknown
    Breastfeeding is not recommended.

Patients should have baseline pulmonary function tests with arterial blood gases, thallium stress tests to exclude the presence of significant coronary artery disease, and brain imaging to exclude metastases. Patients who have had a nephrectomy are still eligible for treatment if they have serum creatinine levels within normal range. Pre-existing infections must be treated prior to starting aldesleukin.

H - Interactions

Psychotropics (narcotics, sedatives, tranquilizers, antiemetics) Enhances CNS toxicities Additive Caution
Antihypertensives Potentiate hypotension Additive Caution; monitor blood pressure
Radiographic iodinated contrast media non-anaphylactic hypersensitivity Unknown Caution
Glucocorticoids ↓ anti-tumour effect of aldesleukin Unknown Avoid, but may be needed to manage side effects
cytotoxics Potentiate myelosuppression, TLS Additive Caution
Nephrotoxic drugs (i.e. aminoglycosides, amphotericin B, methotrexate) potentiate renal toxicity Additive (possibly) Caution
Hepatotoxic agents (e.g., methotrexate, asparaginase) potentiate hepatotoxicity Additive (possibly) Caution
Cardiotoxic agents (e.g., doxorubicin) Potentiate cardiotoxicity Additive (possibly) Caution
DTIC, cisplatin, interferon, tamoxifen ↑ hypersensitivity Additive Caution
Interferon ↑ hypersensitivity, cardiotoxicity and rhabdomyolysis, autoimmune disease Unknown Caution
Drug excreted via liver or kidney ↓ excretion ↓ renal, liver function Caution
I - Recommended Clinical Monitoring

Treating physicians may decide to monitor more or less frequently for individual patients but should always consider recommendations from the product monograph.

Refer to the hepatitis B virus screening and management guideline for monitoring during and after treatment.

Recommended Clinical Monitoring

Monitor Type Monitor Frequency
CBC Baseline and frequent
Electrolytes, blood glucose Baseline and frequent
Liver function tests Baseline and frequent
Renal function tests, fluid intake and output Baseline and frequent
Pulmonary function tests with arterial blood gases (FEV1 > 2L or ≥ 75% of predicted for age) Baseline
CT scan of brain to exclude CNS metastases Baseline
Thallium stress tests to exclude significant coronary artery disease Baseline
Frequent weight, vital signs, EKG etc. during treatment
Chest x-ray Baseline and regular
Clinical toxicity assessment for GI, hydration, cardiovascular, CNS, perfusion, autoimmune effects regular

Grade toxicity using the current NCI-CTCAE (Common Terminology Criteria for Adverse Events) version

Suggested Clinical Monitoring

Monitor Type Monitor Frequency
  • Repeat thallium testing if suspicion of ischemia or congestive cardiac failure
  • Constant cardiac rhythm monitoring and hourly vital signs in patients with hypotension, especially bp < 90 mmHg
J - Supplementary Public Funding

New Drug Funding Program (NDFP Website )

  • Aldesleukin (interleukin-2) - In-Transit Metastases from Melanoma

K - References

McEvoy GK, editor. AHFS Drug Information 2009. Bethesda: American Society of Health-System Pharmacists, p. 915-24.

Proleukin® (aldesleukin/interleukin-2) [product monograph]. Dorval, Quebec: Novartis Pharmaceuticals Canada Inc.; Sept 20, 2012.

April 2024 Updated pregnancy/breastfeeding section

L - Disclaimer

Refer to the New Drug Funding Program or Ontario Public Drug Programs websites for the most up-to-date public funding information.

The information set out in the drug monographs, regimen monographs, appendices and symptom management information (for health professionals) contained in the Drug Formulary (the "Formulary") is intended for healthcare providers and is to be used for informational purposes only. The information is not intended to cover all possible uses, directions, precautions, drug interactions or adverse effects of a particular drug, nor should it be construed to indicate that use of a particular drug is safe, appropriate or effective for a given condition. The information in the Formulary is not intended to constitute or be a substitute for medical advice and should not be relied upon in any such regard. All uses of the Formulary are subject to clinical judgment and actual prescribing patterns may not follow the information provided in the Formulary.

The format and content of the drug monographs, regimen monographs, appendices and symptom management information contained in the Formulary will change as they are reviewed and revised on a periodic basis. The date of last revision will be visible on each page of the monograph and regimen. Since standards of usage are constantly evolving, it is advised that the Formulary not be used as the sole source of information. It is strongly recommended that original references or product monograph be consulted prior to using a chemotherapy regimen for the first time.

Some Formulary documents, such as the medication information sheets, regimen information sheets and symptom management information (for patients), are intended for patients. Patients should always consult with their healthcare provider if they have questions regarding any information set out in the Formulary documents.

While care has been taken in the preparation of the information contained in the Formulary, such information is provided on an “as-is” basis, without any representation, warranty, or condition, whether express, or implied, statutory or otherwise, as to the information’s quality, accuracy, currency, completeness, or reliability.

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