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Keytruda

pembrolizumab
PD-1 Inhibitor FDA Approved 2014 Merck & Co.
1. Indications and Usage

Melanoma (adjuvant and unresectable/metastatic); Non-small cell lung cancer (NSCLC) — first-line monotherapy (PD-L1 TPS ≥1%), first-line combination with chemo, after progression on platinum chemo; Small cell lung cancer; Head and neck squamous cell carcinoma; Classical Hodgkin lymphoma; Primary mediastinal large B-cell lymphoma; Urothelial carcinoma; Microsatellite instability-high (MSI-H) or mismatch repair deficient (dMMR) solid tumors; Gastric/GEJ adenocarcinoma; Esophageal cancer; Cervical cancer; Hepatocellular carcinoma; Merkel cell carcinoma; Renal cell carcinoma; Endometrial carcinoma; Tumor mutational burden-high (TMB-H) solid tumors; Cutaneous squamous cell carcinoma; Triple-negative breast cancer; Biliary tract cancer

2. Dosage and Administration

Adults: 200 mg IV every 3 weeks OR 400 mg IV every 6 weeks until disease progression, unacceptable toxicity, or up to 24 months in patients without disease progression.
Pediatric (MSI-H/dMMR): 2 mg/kg (up to 200 mg) IV every 3 weeks.
Infusion time: Administer over 30 minutes.

3. Dosage Forms and Strengths

Injection: 25 mg/mL solution in 4 mL single-dose vial (100 mg); Lyophilized powder: 50 mg in single-dose vial for reconstitution

4. Contraindications

No absolute contraindications are listed in the prescribing information. Use is contraindicated in patients with known severe hypersensitivity to pembrolizumab or any component of the formulation.

5. Warnings and Precautions
  • Immune-Mediated Adverse Reactions: Pembrolizumab can cause immune-mediated pneumonitis, colitis, hepatitis, endocrinopathies (including hypophysitis, thyroid disorders, type 1 diabetes mellitus, adrenal insufficiency), nephritis, dermatologic reactions, and other immune-mediated adverse reactions.
  • Infusion-Related Reactions: Severe and life-threatening infusion-related reactions have been reported.
  • Complications of Allogeneic HSCT: Fatal and other serious complications can occur in patients who receive allogeneic HSCT before or after anti-PD-1 therapy.
  • Embryo-Fetal Toxicity: Can cause fetal harm based on mechanism of action.
6. Adverse Reactions
Most Common Adverse Reactions

Fatigue (34%), musculoskeletal pain (22%), rash (22%), diarrhea (22%), pruritus (20%), decreased appetite (16%), nausea (16%), cough (15%), pyrexia (13%), constipation (12%), hypothyroidism (12%)

Fatigue
34%
Musculoskeletal Pain
22%
Rash
22%
Diarrhea
22%
Pruritus
20%
Decreased Appetite
16%
Nausea
16%
Cough
15%
Pyrexia
13%
Constipation
12%
Serious Adverse Reactions

Immune-mediated pneumonitis (3.4%), immune-mediated colitis (2.3%), immune-mediated hepatitis (1.3%), immune-mediated nephritis (0.7%), severe skin reactions (1.7%)

Consult the complete prescribing information for a comprehensive list of adverse reactions and their frequencies.

7. Drug Interactions

No formal pharmacokinetic drug interaction studies have been conducted with pembrolizumab. Systemic corticosteroids or immunosuppressants should be avoided before starting pembrolizumab due to potential interference with pharmacodynamic activity.

8. Use in Specific Populations
Pregnancy

Category D equivalent — Can cause fetal harm. Verify pregnancy status prior to initiation. Advise females of reproductive potential to use effective contraception during treatment and for 4 months after the last dose.

Pediatric Use

Safety and effectiveness established for MSI-H/dMMR cancers in pediatric patients. Not established for other indications in patients <18 years.

Renal/Hepatic Impairment

No dose adjustment recommended for mild or moderate renal impairment. Not studied in severe renal impairment. No dose adjustment for mild hepatic impairment (bilirubin ≤ULN with AST >ULN, or bilirubin >1 to 1.5× ULN). Not studied in moderate or severe hepatic impairment.

12. Clinical Pharmacology
Mechanism of Action

Pembrolizumab is a humanized monoclonal antibody that binds to the programmed death-1 (PD-1) receptor on T cells, blocking its interaction with ligands PD-L1 and PD-L2. This releases PD-1 pathway-mediated inhibition of the immune response, including the anti-tumor immune response, thereby restoring T-cell-mediated killing of tumor cells.

Pharmacokinetics

Steady-state concentration reached by 16 weeks with repeated dosing every 3 weeks. Terminal half-life: approximately 22 days. Volume of distribution: 6.0 L. Clearance: 0.22 L/day.

14. Clinical Studies

Clinical efficacy and safety data supporting the approval of Keytruda are available in the full prescribing information and from the clinical trials listed below.

Pivotal Clinical Trials
Additional Resources
FDA-Approved Tumor Types
External Resources
Important Notice: This page is intended as a navigational reference to the FDA-approved prescribing information for Keytruda. It does not replace the full prescribing information. Healthcare professionals should consult the complete package insert available at DailyMed before making prescribing decisions. Patient-specific factors should always guide clinical decision-making.