Overview
Pembrolizumab is a highly selective IgG4-kappa humanized monoclonal antibody against PD-1 receptors. It was generated by grafting the variable sequences of a very high-affinity mouse antihuman PD-1 antibody onto a human IgG4-kappa isotype containing a stabilizing S228P Fc mutation. It contains 32 cysteine residues and the complete folded molecule includes 4 disulfide linkages as interchain bonds and 23 interchain bonds. It was developed by Merck & Co and first approved for the treatment of metastatic malignant melanoma by the FDA on September 4, 2014, becoming the first approved therapy against PD-1. In the time since its initial approval, pembrolizumab has been granted approval in the treatment of a wide variety of cancers.
Indication
Pembrolizumab is indicated for the following conditions: For all approved adult indications, pembrolizumab may be used for an additional 6 weeks at 400mg weekly.
Associated Conditions
- Advanced Endometrial Cancer
- Advanced Renal Cell Carcinoma
- Hepatocellular Carcinoma
- Locally Advanced Cutaneous Squamous Cell Carcinoma
- Locally Advanced or Metastatic Urothelial Carcinoma (UC)
- Metastatic Adenocarcinoma of the Gastroesophageal Junction
- Metastatic Cervical Cancer
- Metastatic Esophageal Carcinoma
- Metastatic Melanoma
- Metastatic Non-Small Cell Lung Cancer
- Metastatic Renal Cell Carcinoma ( mRCC)
- Metastatic Squamous Cell Carcinoma of the Head and Neck (HNSCC)
- Metastatic Triple Negative Breast Cancers
- Metastatic Urothelial Carcinoma (UC)
- Metastatic cutaneous squamous cell carcinoma
- Metastic Renal Cell Carcinoma
- Non-Small Cell Lung Cancer (NSCLC)
- Nonsmall Cell Lung Cancer, Stage II
- Persistent Cervical Cancer
- Recurrent Cervical Cancer
- Refractory Primary Mediastinal Large B-Cell Cell Lymphoma
- Renal Cell Carcinoma (RCC)
- Resectable Non-small Cell Lung Cancer
- Stage IB Non-small Cell Lung Cancer
- Stage IIB Melanoma
- Stage IIC Melanoma
- Stage III Melanoma
- Stage IIIA Non Small Cell Lung Cancer
- Unresectable Melanoma
- Advanced Microsatellite Instability High Endometrial Carcinoma
- Advanced Mismatch Repair-deficient (dMMR) Endometrial Carcinoma
- High risk, early Triple Negative Breast Cancer
- High risk, in situ Non-Muscle Invasive Bladder Cancer (NMIBC) Refractory to BCG
- Locally advanced Adenocarcinomas of the Gastroesophageal Junction
- Locally advanced Esophageal Carcinoma
- Locally advanced Urothelial Carcinoma
- Metastatic HER2-positive Adenocarcinoma of the Stomach
- Metastatic HER2-positive Adenocarcinomas of the Gastroesophageal Junction
- Metastatic High Tumor Mutation Burden Solid Tumors
- Metastatic Merkel Cell Carcinoma (MCC)
- Metastatic Microsatellite Instability High Colorectal Cancer
- Metastatic Microsatellite Instability-High (MSI-H) Solid Tumors
- Metastatic Mismatch Repair Deficient Colorectal Cancer
- Metastatic Mismatch repair deficient (dMMR) solid tumors
- Recurrent Cutaneous Squamous Cell Carcinoma
- Recurrent Squamous Cell Carcinoma of the Head and Neck (SCCHN)
- Recurrent, locally advanced Adenocarcinomas of the Gastroesophageal Junction
- Recurrent, locally advanced Merkel Cell Carcinoma
- Refractory Classical Hodgkin's Lymphoma
- Relapsed Classical Hodgkin's Lymphoma
- Stage 3 Non-Small Cell Lung Carcinoma (NSCLC)
- Unresectable High Tumor Mutation Burden Solid Tumors
- Unresectable Microsatellite Instability High Colorectal Cancer
- Unresectable Microsatellite Instability-High (MSI-H) Solid Tumors
- Unresectable Mismatch Repair Deficient Colorectal Cancer
- Unresectable Mismatch repair deficient (dMMR) solid tumors
- Unresectable, locally advanced HER2-positive Adenocarcinoma of the Stomach
- Unresectable, locally advanced HER2-positive Adenocarcinomas of the Gastroesophageal Junction
- Unresectable, locally recurrent Triple Negative Breast Cancer
- Unresectable, recurrent Squamous Cell Carcinoma of the Head and Neck (SCCHN)
Research Report
Pembrolizumab: A Comprehensive Oncological Review
I. Introduction to Pembrolizumab
A. Overview and Generic Information
Pembrolizumab, marketed internationally under the brand name Keytruda, is a cornerstone of modern cancer immunotherapy. It is a humanized monoclonal antibody designed to harness the patient's own immune system to combat various malignancies.[1]
- Generic Name: Pembrolizumab.[1]
- DrugBank ID: DB09037.[14]
- CAS Number: 1374853-91-4 [User Query].
- Type: Pembrolizumab is classified as a biotechnology-derived product (Biotech).[14]
- Brief Summary of Therapeutic Use: As a programmed death receptor-1 (PD-1) blocking antibody, Pembrolizumab is indicated for the treatment of numerous cancer types. Its primary function is to restore the immune system's ability to detect and destroy tumor cells.[1] Initial indications included advanced melanoma and non-small cell lung cancer, with subsequent approvals for head and neck cancer, Hodgkin's lymphoma, cervical cancer, and many others [User Query].
- Developer: Merck & Co., Inc. (known as MSD outside the United States and Canada) is the developer of Pembrolizumab.[4] Merck's extensive and ongoing KEYNOTE clinical trial program has been pivotal in establishing the broad efficacy and safety profile of Pembrolizumab across a multitude of cancer indications and treatment settings.[85]
B. Significance in Immuno-Oncology
Pembrolizumab achieved a landmark FDA approval on September 4, 2014, for patients with advanced melanoma, making it the first anti-PD-1 therapy to reach the U.S. market.[4] This heralded a new era in cancer treatment.
Clinical Trials
Title | Posted | Study ID | Phase | Status | Sponsor |
|---|---|---|---|---|---|
2025/07/08 | Not Applicable | Not yet recruiting | |||
2025/06/25 | Phase 2 | Not yet recruiting | City of Hope Medical Center | ||
2025/06/18 | Phase 3 | Not yet recruiting | |||
2025/06/18 | Phase 2 | Not yet recruiting | |||
2025/06/15 | Phase 2 | Not yet recruiting | Michael Spinner, MD | ||
2025/06/12 | Phase 2 | Not yet recruiting | |||
2025/06/12 | Phase 2 | Not yet recruiting | |||
2025/06/11 | Phase 2 | Not yet recruiting | Stephen Shiao | ||
2025/06/11 | Phase 2 | Not yet recruiting | Vandana Abramson | ||
2025/06/10 | Phase 2 | Not yet recruiting |
FDA Drug Approvals
Approved Product | Manufacturer | NDC Code | Route | Strength | Effective Date |
|---|---|---|---|---|---|
| Merck Sharp & Dohme LLC | 0006-3026 | INTRAVENOUS | 25 mg in 1 mL | 3/11/2024 | |
| Merck Sharp & Dohme LLC | 0006-3029 | INTRAVENOUS | 50 mg in 2 mL | 3/11/2024 |
EMA Drug Approvals
Approved Product | Authorization Holder | Status | Issued Date |
|---|---|---|---|
Authorised | 7/17/2015 |
HSA Drug Approvals
Approved Product | Manufacturer | Approval Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| KEYTRUDA SOLUTION FOR INFUSION 25MG/ML | SIN14881P | INFUSION, SOLUTION CONCENTRATE | 25.0 mg/mL | 10/27/2015 | |
| Pembrolizumab Solution for Infusion 25mg/mL | SIN16677P | INFUSION, SOLUTION CONCENTRATE | 25.0mg/mL | 1/13/2023 |
NMPA Drug Approvals
Approved Product | Company | Approval Number | Drug Type | Dosage Form | Approval Date |
|---|---|---|---|---|---|
| Pembrolizumab injection | 国药准字SJ20180019 | 生物制品 | 注射剂 | 12/22/2022 |
PPB Drug Approvals
Approved Product | Registration No. | Company | Licence No. | Strength | Registration Date |
|---|---|---|---|---|---|
| No PPB approvals found for this drug. | |||||
TGA Drug Approvals
Approved Product | ARTG ID | Sponsor | Registration Type | Status | Registration Date |
|---|---|---|---|---|---|
| KEYTRUDA pembrolizumab (rch) 100mg/4 mL concentrated injection vial | 263932 | Medicine | A | 3/8/2016 |
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