Pembrolizumab
[CAS# 1374853-91-4]

Identification

• Classification: API >> Antineoplastic agents
• Name: Pembrolizumab
• Synonyms: Keytruda; Lambrolizumab; Lanbrolizumab; MK 3475; Merck 3475
• Molecular Formula: C₆₅₀₄H₁₀₀₀₄N₁₇₁₆O₂₀₃₆S₄₆
• Molecular Weight: 146286.29
• Protein Sequence: Heavy Chain Sequence$$nl$$QVQLVQSGVEVKKPGASVKVSCKASGYTFTNYYMYWVRQAPGQGLEWMGGINPSNGGTNF$$nl$$NEKFKNRVTLTTDSSTTTAYMELKSLQFDDTAVYYCARRDYRFDMGFDYWGQGTTVTVSS$$nl$$ASTKGPSVFPLAPCSRSTSESTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSS$$nl$$GLYSLSSVVTVPSSSLGTKTYTCNVDHKPSNTKVDKRVESKYGPPCPPCPAPEFLGGPSV$$nl$$FLFPPKPKDTLMISRTPEVTCVVVDVSQEDPEVQFNWYVDGVEVHNAKTKPREEQFNSTY$$nl$$RVVSVLTVLHQDWLNGKEYKCKVSNKGLPSSIEKTISKAKGQPREPQVYTLPPSQEEMTK$$nl$$NQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSRLTVDKSRWQEG$$nl$$NVFSCSVMHEALHNHYTQKSLSLSLGK$$nl$$$$nl$$Light Chain Sequence$$nl$$EIVLTQSPATLSLSPGERATLSCRASKGVSTSGYSYLHWYQQKPGQAPRLLIYLASYLES$$nl$$GVPARFSGSGSGTDFTLTISSLEPEDFAVYYCQHSRDLPLTFGGGTKVEIKRTVAAPSVF$$nl$$IFPPSDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLS$$nl$$STLTLSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC
• CAS Registry Number: 1374853-91-4
• EC Number: 807-012-2

Properties

• Solubility: 22.5-27.5 mg/ml (histidine buffer)

Safety Data

• Hazard Symbols: GHS08 Danger
• Risk Statements: H360-H372
• Safety Statements: P203-P260-P264-P270-P280-P318-P319-P405-P501

Hazard Classification

Hazard	Class	Category Code	Hazard Statement
Reproductive toxicity	Repr.	1B	H360
Specific target organ toxicity - repeated exposure	STOT RE	1	H372

Discovery and Applications

Pembrolizumab, marketed under the brand name Keytruda, was developed by researchers at Merck & Co. Pembrolizumab belongs to a class of drugs known as immune checkpoint inhibitors, which work by targeting the programmed cell death protein 1 (PD-1) pathway. The discovery of pembrolizumab stemmed from efforts to harness the body's immune system to fight cancer by blocking immune checkpoints.

Pembrolizumab has revolutionized the treatment of various cancers, particularly melanoma, non-small cell lung cancer, and certain types of advanced or metastatic cancers. It has shown remarkable efficacy in patients with tumors that express high levels of PD-L1, leading to durable responses and prolonged survival. Pembrolizumab is administered intravenously and is often used as monotherapy or in combination with other anticancer agents.

References

2013. Safety and Tumor Responses with Lambrolizumab (Anti-PD-1) in Melanoma. The New England Journal of Medicine, 369(2).
DOI: 10.1056/nejmoa1305133

2018. Pembrolizumab plus Chemotherapy for Squamous Non-Small-Cell Lung Cancer. The New England Journal of Medicine, 379(21).
DOI: 10.1056/nejmoa1810865

2019. Pembrolizumab plus Axitinib versus Sunitinib for Advanced Renal-Cell Carcinoma. The New England Journal of Medicine, 380(12).
DOI: 10.1056/nejmoa1816714