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Keytruda (pembrolizumab)
Pembrolizumab blocks PD-1 receptor, releasing immune inhibition and enhancing anti-tumor T-cell response.
KEYTRUDA QLEX combines pembrolizumab (PD-1 inhibitor) with berahyaluronidase alfa for enhanced subcutaneous delivery across multiple cancer indications including melanoma, NSCLC, mesothelioma, and HNSCC. The drug demonstrates clinical efficacy as monotherapy and in combination regimens, with steady-state pharmacokinetics achieved by 16 weeks and a 22-day half-life enabling convenient dosing schedules. Primary contraindication is hypersensitivity to berahyaluronidase alfa or hyaluronidase; specific populations including pediatric patients ≥12 years and those with mild-to-moderate hepatic impairment show comparable pharmacokinetics to adults. Companion diagnostics for PD-L1 expression and EGFR/ALK status are required for appropriate patient selection in NSCLC and HNSCC indications.
At a glance
| Generic name | pembrolizumab |
|---|---|
| Sponsor | Merck & Co. |
| Drug class | Monoclonal antibody; PD-1 inhibitor |
| Target | PD-1 receptor |
| Modality | Monoclonal antibody |
| Therapeutic area | Oncology |
| Phase | FDA-approved |
| First approval | 2014 |
| Annual revenue | 29500 |
Mechanism of action
Pembrolizumab is a monoclonal antibody that binds to the PD-1 receptor on T cells and blocks its interaction with PD-L1 and PD-L2 ligands. This blockade releases PD-1 pathway-mediated inhibition of the immune response, including anti-tumor immunity. Upregulation of PD-1 ligands occurs in some tumors and normally contributes to inhibition of active T-cell immune surveillance; pembrolizumab reverses this mechanism. Berahyaluronidase alfa is an endoglycosidase variant of human hyaluronidase PH20 that temporarily and locally breaks down hyaluronan in the subcutaneous tissue extracellular matrix. This increases tissue permeability to facilitate drug delivery. The effects are reversible, with tissue permeability restored within 24 to 48 hours. In preclinical models, blocking PD-1 activity decreased tumor growth. Combination treatment with a PD-1 blocking antibody and lenvatinib kinase inhibitor decreased tumor-associated macrophages, increased activated cytotoxic T cells, and reduced tumor growth compared to either treatment alone.
Approved indications
- Melanoma
- NSCLC (nonsquamous)
- NSCLC (squamous)
- NSCLC (PD-L1+)
- NSCLC (PD-L1+, post-platinum)
- NSCLC (neoadjuvant)
- NSCLC (adjuvant)
- MPM
- HNSCC (PD-L1+)
- HNSCC (first-line)
- HNSCC (PD-L1+, post-platinum)
- HNSCC (post-platinum)
- Urothelial Cancer
- Urothelial Cancer (platinum-ineligible)
- Urothelial Cancer (MIBC, neoadjuvant)
- Urothelial Cancer (BCG-unresponsive)
Common side effects
- Nausea
- Fatigue
- Anaemia
- Diarrhoea
- Constipation
- Decreased appetite
- Hypothyroidism
- Vomiting
- Pruritus
- Arthralgia
- Hypertension
- Alanine aminotransferase increased
Key clinical trials
- Study of Two Doses of Pembrolizumab (MK-3475) Versus Docetaxel in Previously Treated Participants With Non-Small Cell Lung Cancer (MK-3475-010/KEYNOTE-010) (PHASE2, PHASE3)
- Study to Evaluate the Safety and Efficacy of Two Different Dosing Schedules of Pembrolizumab (MK-3475) Compared to Ipilimumab in Participants With Advanced Melanoma (MK-3475-006/KEYNOTE-006) (PHASE3)
- Study of Pemetrexed+Platinum Chemotherapy With or Without Pembrolizumab (MK-3475) in Participants With First Line Metastatic Nonsquamous Non-small Cell Lung Cancer (MK-3475-189/KEYNOTE-189) (PHASE3)
- A Study of Carboplatin-Paclitaxel/Nab-Paclitaxel Chemotherapy With or Without Pembrolizumab (MK-3475) in Adults With First Line Metastatic Squamous Non-small Cell Lung Cancer (MK-3475-407/KEYNOTE-407) (PHASE3)
- Study of Pembrolizumab (MK-3475) Versus Chemotherapy in Participants With Advanced Melanoma (MK-3475-002/P08719/KEYNOTE-002) (PHASE2)
- Study of Pembrolizumab (MK-3475) in Participants With Advanced Urothelial Cancer (MK-3475-052/KEYNOTE-052) (PHASE2)
- Study of Pembrolizumab (MK-3475) Compared to Platinum-Based Chemotherapies in Participants With Metastatic Non-Small Cell Lung Cancer (MK-3475-024/KEYNOTE-024) (PHASE3)
- Study of Pembrolizumab (MK-3475) in Participants With Advanced Solid Tumors (MK-3475-012/KEYNOTE-012) (PHASE1)
Patents
| Patent | Expiry | Type |
|---|---|---|
| Biologic Exclusivity |
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
| FDA Orange Book | Patents + exclusivity |
| SEC EDGAR | Revenue + earnings |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Keytruda CI brief — competitive landscape report
- Keytruda updates RSS · CI watch RSS
- Merck & Co. portfolio CI