Monoclonal antibody | |
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Type | Whole antibody |
Source | Chimeric |
Target | CA-IX |
Clinical data | |
Trade names | Rencarex |
ATC code |
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Identifiers | |
CAS Number | |
ChemSpider |
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UNII | |
Chemical and physical data | |
Formula | C6460H10006N1718O2018S48 |
Molar mass | 145566.00 g·mol−1 |
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Girentuximab (trade name Rencarex) is a chimeric IgG1 monoclonal antibody to carbonic anhydrase IX (CAIX). [1] CAIX is expressed on the surface of most renal cancer cells and is hypothesized to be on the surface of other tumor cells. It is investigational agent in clinical trials for renal cell carcinoma. [2] Its development was suspended as a "naked" or unconjugated antibody during phase III trials due to efficacy. [3] [4]
Girentuximab was originally developed by Wilex AG, Germany. It was granted fast track status and orphan drug designation by the FDA for renal cancer. [5] In January 2017, Telix Pharmaceuticals Limited, an Australian biotechnology company, announced that it had in-licensed Girentuximab for use as a radioimmunoconjugate. [6]
It triggers antibody-dependent cell-mediated cytotoxicity (ADCC). When it binds to its antigen (carbonic anhydrase IX), it activates natural killer cells by binding to a receptor on the NK cells. [7]
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Carbonic anhydrase IX is an enzyme that in humans is encoded by the CA9 gene. It is one of the 14 carbonic anhydrase isoforms found in humans and is a transmembrane dimeric metalloenzyme with an extracellular active site that facilitates acid secretion in the gastrointestinal tract. CA IX is overexpressed in many types of cancer including clear cell renal cell carcinoma (RCC) as well as carcinomas of the cervix, breast and lung where it promotes tumor growth by enhancing tumor acidosis.
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