Generic
Pembrolizumab
1 brands available in the market
At a glance
Pembrolizumab is a programmed death receptor-1 (PD-1)-blocking antibody used for the treatment of melanoma, non-small cell lung cancer, head and neck cancer, cervical cancer, and various other cancers.
Description
Pembrolizumab is a humanized immunoglobulin G4 monoclonal antibody that binds to the cell surface receptor programmed death-1 (PD-1) and prevents it from interacting with ligands PD-L1 and PD-L2. Blockade of the PD-1 pathway results in the reactivation of T-lymphocytes and induction of immune response to tumor cells.
Indications
- Melanoma (unresectable or metastatic)
- Non-Small Cell Lung Cancer (NSCLC)
- Small Cell Lung Cancer (SCLC)
- Head and Neck Squamous Cell Cancer (HNSCC)
- Classical Hodgkin Lymphoma (cHL)
- Primary Mediastinal Large B-Cell Lymphoma (PMBCL)
- Urothelial Carcinoma
- Microsatellite Instability-High (MSI-H) Cancer
- Gastric Cancer
- Esophageal Cancer
- Cervical Cancer
- Hepatocellular Carcinoma (HCC)
- Merkel Cell Carcinoma (MCC)
- Renal Cell Carcinoma (RCC)
- Endometrial Carcinoma
Therapeutic class
Immunological Chemotherapy, Immunosuppressant
Pharmacological class
PD-1/PD-L1 Inhibitor (Immune Checkpoint Inhibitor)
Pharmacology
Pembrolizumab is a monoclonal antibody that binds to the PD-1 receptor and blocks its interaction with PD-L1 and PD-L2, releasing PD-1 pathway-mediated inhibition of the immune response, including the anti-tumor immune response. In syngeneic mouse tumor models, blocking PD-1 activity resulted in decreased tumor growth.
Mechanism of action
Binds to PD-1 receptor to block the PD-1 pathway, reactivating T-cell-mediated anti-tumor immune responses.
Dosage
Adult Dose (Intravenous):
- Most indications: 200 mg once every 3 weeks as 30-minute IV infusion
- Pediatric (cHL, PMBCL, MSI-H, MCC): 2 mg/kg (up to 200 mg) every 3 weeks
- RCC: With axitinib 5 mg orally twice daily
- Endometrial Carcinoma: With lenvatinib 20 mg orally once daily (not MSI-H or dMMR)
- Until disease progression or unacceptable toxicity, or up to 24 months (35 cycles) without disease progression
Administration
- Administered by doctor or nurse as 30-minute IV infusion
- Do not self-administer
- Once every 3 weeks
Missed dose
If you miss a dose, consult your doctor.
Side effects
Common Side Effects (≥20%):
- Fatigue
- Musculoskeletal pain
- Decreased appetite
- Pruritus
- Diarrhea
- Nausea
- Rash
- Pyrexia
- Cough
- Dyspnea
- Constipation
- Abdominal pain
Precautions & warnings
- Immune-mediated pneumonitis, colitis, hepatitis, nephritis, endocrinopathies, skin reactions: Withhold or permanently discontinue based on severity
- Infusion-related reactions: Discontinue for severe/life-threatening reactions
- Complications of allogeneic HSCT: Monitor for GVHD, hepatic veno-occlusive disease
- Treatment of multiple myeloma with PD-1/PD-L1 blocker + thalidomide analogue + dexamethasone not recommended outside controlled trials
- Embryo-fetal toxicity: Potential risk to fetus; use effective contraception
Contraindications
None.
Drug interactions
- Systemic corticosteroids or immunosuppressants may interfere with pembrolizumab efficacy
Food interactions
It is not known whether it is safe to consume alcohol with Pembrolizumab; consult your doctor.
Use in pregnancy
Use in Pregnancy: Can cause fetal harm when administered to a pregnant woman; advise women of potential risk to the fetus.
Pregnancy Category: D — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: No data on presence in human milk; due to potential serious adverse reactions in breastfed infants, advise women not to breastfeed during treatment and for 4 months after the final dose.
Pediatric use
Safety and effectiveness not established in pediatric patients (except specific indications).
Geriatric use
No overall differences in safety or effectiveness observed between elderly and younger patients.
Renal / hepatic impairment
Renal Impairment: Caution in kidney disease; dose adjustment may be needed.
Hepatic Impairment: Caution in liver disease; dose adjustment may be needed.
Overdose effects
No overdose information available; treatment: general supportive measures.
Storage conditions
Store at 2-8°C in the refrigerator; after reconstitution, use within 24 hours.
Chemical structure
Pembrolizumab