Pembrolizumab

DEA Class; Rx

Common Brand Names; Keytruda

• Antineoplastics, Monoclonal Antibody; 
• PD-1/PD-L1 Inhibitors

Melanoma

Unresectable or metastatic melanoma

• Indicated for treatment of unresectable or metastatic melanoma

Adjuvant treatment

• Indicated for adjuvant treatment of adults with Stage IIB, IIC, or III melanoma following complete resection

Non-Small Cell Lung Cancer

Single-agent

• First-line treatment of patients with stage III non-small cell lung cancer (NSCLC), who are not candidates for surgical resection or definitive chemoradiation, or metastatic NSCLC, and whose tumors express PD-L1 [Tumor Proportion Score (TPS) ≥1%)], with no EGFR or ALK genomic tumor aberrations
• Metastatic NSCLC whose tumors with PD-L1 expression (TPS ≥1%) and disease progression on or after platinum-containing chemotherapy; patients with EGFR or ALK genomic tumor aberrations should have disease progression on FDA-approved therapy for these aberrations prior to receiving pembrolizumab

Combination therapy

• Metastatic nonsquamous NSCLC: First-line treatment in combination with pemetrexed and platinum chemotherapy with no EGFR or ALK genomic tumor aberrations
• Metastatic squamous NSCLC: First-line treatment in combination with carboplatin and either paclitaxel or paclitaxel protein bound

Head & Neck Squamous Cell Carcinoma

Single-agent therapy

• Indicated for first-line treatment of patients with metastatic or with unresectable, recurrent HNSCC whose tumors express PD-L1 [Combined Positive Score (CPS) ≥1]
• Indicated for treatment of patients with recurrent or metastatic HNSCC with disease progression on or after platinum-containing chemotherapy

Combination therapy

• Indicated in combination with platinum and fluorouracil (FU) for the first-line treatment of patients with metastatic or with unresectable, recurrent HNSCC

Indicated for relapsed or refractory classical Hodgkin lymphoma (cHL)

Indicated for refractory primary mediastinal large B-cell lymphoma (PMBCL), or who have relapsed after ≥2 prior lines of therapy

Urothelial Carcinoma

Locally advanced or metastatic urothelial carcinoma

• Indicated for locally advanced or metastatic urothelial carcinoma in patients who are ineligible for any platinum-containing chemotherapy or have disease progression during or following platinum-containing chemotherapy or within 12 months of neoadjuvant or adjuvant treatment with platinum-containing chemotherapy

Bacillus Calmette-Guerin (BCG)-unresponsive bladder cancer

• Indicated for treatment of BCG-unresponsive, high-risk, nonmuscle invasive bladder cancer (NMIBC) with carcinoma in situ (CIS) with or without papillary tumors in patients who are ineligible for, or have elected not to undergo cystectomy

Indicated for unresectable or metastatic, microsatellite instability-high (MSI-H) or mismatch repair deficient (dMMR) who have solid tumors that have progressed following prior treatment and in patients who have no satisfactory alternative treatment options

Indicated for unresectable or metastatic MSI-H or dMMR colorectal cancer (CRC)

Indicated in combination with trastuzumab, fluoropyrimidine- and platinum-containing chemotherapy, for first-line treatment of patients with locally advanced unresectable or metastatic HER2-positive gastric or gastroesophageal junction (GEJ) adenocarcinoma

Indicated for recurrent locally advanced or metastatic esophageal or gastroesophageal junction (GEJ) (tumors with epicenter 1-5 cm above GEJ) carcinoma in patients who are not candidates for surgical resection or definitive chemoradiation

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• Hyperglycemia (45%)
• Hypertriglyceridemia (43%)
• Anemia (3%)
• Lymphopenia (33%)
• Hyponatremia (28%)
• Fatigue (28%)
• Increased AST (27%)
• Hypoalbuminemia (27%)
• Rash (24%)
• Increased ALT (23%)
• Increased alkaline phosphatase (21%)
• Hypercholesterolemia (20%)
• Arthralgia (18%)
• Cough (17%)
• Decreased appetite (16%)
• Headache (14%)
• Vitiligo (13%)
• Back pain (12%)
• Dyspnea (11%)

Monitor for signs and symptoms of adrenal insufficiency; administer corticosteroids and hormone replacement as clinically indicated; withhold therapy for moderate (Grade 2) adrenal insufficiency and withhold or discontinue for severe (Grade 3) or life-threatening (Grade 4) adrenal insufficiency

Solid organ transplant rejection reported in postmarketing setting; treatment increases risk of rejection in solid organ transplant recipients; consider benefit of treatment versus risk of possible organ rejection

Infusion-related reactions, including severe and life-threatening reactions, reported; monitor for signs and symptoms of infusion-related reactions including rigors, chills, wheezing, pruritus, flushing, rash, hypotension, hypoxemia, and fever; interrupt or slow rate of infusion for mild (Grade 1) or moderate (Grade 2) infusion-related reactions; for severe (Grade 3) or life-threatening (Grade 4) infusion-related reactions, stop infusion and permanently discontinue therapy

Hypophysitis reported; monitor for signs and symptoms of hypophysitis (including hypopituitarism and adrenal insufficiency)

Thyroid disorders can occur; monitor for changes in thyroid function (at the start of treatment, periodically during treatment, and as clinically indicated) and for clinical signs and symptoms of thyroid disorders

Based on its mechanism of action, fetal harm may occur when administered to a pregnant woman (see Pregnancy)

In two randomized clinical trials in patients with multiple myeloma, the addition of pembrolizumab to a thalidomide analogue plus dexamethasone resulted in increased mortality; treatment of patients with multiple myeloma with a PD-1 or PDL1 blocking antibody in combination with a thalidomide analogue plus dexamethasone is not recommended outside of controlled clinical trials

Based on its mechanism of action, fetal harm may occur when administered to a pregnant woman

No human data available informing the risk of embryo-fetal toxicity

Unknown if distributed in human breast milk

No studies conducted to assess impact of pembrolizumab on milk production or its presence in breast milk

Pembrolizumab 

injectable solution

• 100mg/4mL (25mg/mL)