Pertuzumab
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Pertuzumab
| Monoclonal antibody | |
|---|---|
| Type | Whole antibody |
| Source | Humanized (from mouse) |
| Target | HER2 |
| Clinical data | |
| Pregnancy cat. | ? |
| Legal status | ? |
| Identifiers | |
| CAS number | 380610-27-5  |
| ATC code | None |
| UNII | K16AIQ8CTM  |
| KEGG | D05446 |
| Chemical data | |
| Formula | ? |
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Pertuzumab (also called 2C4, trade name Omnitarg) is a monoclonal antibody. The first of its class in a line of agents called "HER dimerization inhibitors". By binding to HER2, it inhibits the dimerization of HER2 with other HER receptors, which is hypothesized to result in slowed tumor growth.[1] Pertuzumab is currently being developed by Genentech. Roche acquired Genentech in 2009 and now owns the IP on Pertuzumab.
Early clinical trials of pertuzumab in prostate, breast, and ovarian cancers have been met with limited success.[2]
The dosage of pertuzumab used in the pivotal phase III CLEOPATRA (Clinical Evaluation of Pertuzumab and Trastuzumab) trial was as follows: IV 840mg loading dose followed by IV 420mg q3w.[3]
The pharmacokinetics of intravenous pertuzumab appear to be unaffected by age and no drug-drug interaction has been reported with docetaxel. The pharmacokinetics and pharmacodynamics of pertuzumab have recently been summarized in a review by Gillian Keating.[3]
The combination of pertuzumab plus trastuzumab plus docetaxel, as compared with placebo plus trastuzumab plus docetaxel, when used as first-line treatment for HER2-positive metastatic breast cancer, significantly prolonged progression-free survival, with no increase in cardiac toxic effects in the randomized, double-blind, multinational, phase III CLEOPATRA trial.[4]
Intravenous pertuzumab is currently being evaluated in patients with breast cancer in the following trials: MARIANNE (advanced breast cancer), NEOSPHERE (early breast cancer), TRYPHAENA (HER2-positive stage II/III breats cancer) and APHINITY (HER2-positive nonmetastatic breast cancer).[3]
References
- ^ de Bono, Johann S.; Bellmunt, J; Attard, G; Droz, JP; Miller, K; Flechon, A; Sternberg, C; Parker, C et al (20 January 2007). "Open-Label Phase II Study Evaluating the Efficacy and Safety of Two Doses of Pertuzumab in Castrate Chemotherapy-Naive Patients With Hormone-Refractory Prostate Cancer". Journal of Clinical Oncology 25 (3): 257–262. doi:10.1200/JCO.2006.07.0888. PMID 17235043.
- ^ Genentech press release - May 15, 2005
- ^ a b c Keating GM. Pertuzumab: in the first-line treatment of HER2-positive metastatic breast cancer. Drugs 2012 Feb 12; 72 (3): 353-60.Link text
- ^ Baselga J, Cortés J, Kim SB, and the CLEOPATRA Study Group. Pertuzumab plus trastuzumab plus docetaxel for metastatic breast cancer. N Engl J Med 2012 Jan 12; 366 (2): 109-19. Link text
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10.1056/NEJMoa1113216
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