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Pembrolizumab

Pembrolizumab
Monoclonal antibody
Type Whole antibody
Source Humanized (from mouse)
Target PD-1
Clinical data
Trade names Keytruda
Pregnancy
category
  • not for pregnant women
Routes of
administration
IV
ATC code
Legal status
Legal status
  • Approved (US)
Identifiers
CAS Number
PubChem SID
DrugBank
ChemSpider
  • none
UNII
Chemical and physical data
Formula C6534H10004N1716O2036S46
Molar mass 146 kDa

Pembrolizumab (formerly MK-3475 and lambrolizumab, trade name Keytruda) is a humanized antibody used in cancer immunotherapy. It destroys a protective mechanism on cancer cells, and allows the immune system to destroy those cancer cells. It targets the programmed cell death 1 (PD-1) receptor. The drug was initially used in treating metastatic melanoma.

As of 2016, pembrolizumab is used via intravenous infusion to treat inoperable or metastatic melanoma, metastatic non-small cell lung cancer (NSCLC) in certain situations, and as a second-line treatment for head and neck squamous cell carcinoma (HNSCC), after platinum-based chemotherapy.

For melanoma, ipilimumab lengthened survival and a subset of patients were surviving after 3 years. In a phase III trial, overall survival for melanoma patients with ipilimumab was 10 months, compared to 6.4 months for patients with conventional (glycoprotein 1000) treatment. In pooled data from 12 trials, survival reached a plateau of 22% after 3 years, suggesting a durable overall survival.

For NSCLC, pembrolizumab is a first line treatment if the cancer overexpresses PDL1 and the cancer has no mutations in EGFR or in ALK; if chemotherapy has already been administered, then pembrolizumab can be used a second line treatment but if the cancer has EGFR or ALK mutations, agents targeting those mutations should be used first. Assessment of PDL1 must be conducted with a validated and approved companion diagnostic.

Women of child-bearing age should use contraception when taking pembrolizumab; it should not be administered to pregnant women because animal studies have shown that it can reduce tolerance to the fetus and increases the risk of miscarriage. It is not known if pembrolizumab is secreted into breast milk or not.

As of 2016, the drug had not been tested in people with active infections including any HIV, hepatitis B or hepatitis C infection, kidney or liver disease, active CNS metastases, active systemic autoimmune disease, interstitial lung disease; prior pneumonia, and people with a history of severe reaction to another monoclonal antibody.


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