Emactuzumab
Humanized (from mouse) | |
Target | CSF1R |
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Clinical data | |
Other names | RG7155, RO5509554 |
Routes of administration | intravenous infusion |
ATC code |
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Pharmacokinetic data | |
Elimination half-life | 1.5 - 9 days |
Identifiers | |
CAS Number | |
DrugBank | |
UNII | |
KEGG | |
Chemical and physical data | |
Formula | C6398H9908N1704O2020S44 |
Molar mass | 144430.19 g·mol−1 |
Emactuzumab
History
Emactuzumab was originally developed by
Mechanism of action
Emactuzumab is a humanized monoclonal antibody directed against the
Clinical efficacy
In a Phase Ib clinical study, biopsies were taken from TGCT subjects before and on emactuzumab treatment, and immunohistochemistry was performed with antibodies against CD68/CD163 (biomarkers for TAMs) and CSF-1R. Altogether, 36 patients (57%) had evaluable paired tumour biopsy samples (taken at baseline and on treatment at four weeks, after two cycles of emactuzumab at doses of 900 – 2000 mg). A significant reduction of >50% of CD68/CD163-positive macrophages and CSF1R-positive macrophages was seen in 22 patients (61%), showing that the neutralisation of CSF-1R by emactuzumab resulted in the concomitant depletion of TAMs. In the efficacy cohort, 45 of 63 patients (71%) had a best overall response of complete response or partial response (PR) and the disease control rate was 98% (62 of 63 patients). None of the patients were assessed with progressive disease at the time of treatment discontinuation, although the majority of patients (39 patients [62%]) only received a limited number of four or five treatment cycles. After one- and two-year follow-up MRI, 19/27 patients (70%) and 9/14 patients (64%), respectively, were still in response at these time points.[8]
References
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- ^ "SynOx Therapeutics raises €37M in Series A Financing". Cision PR Newswire.
- ^ "NCI Drug Dictionary: Emactuzumab". NCI Drug Dictionary. U.S. Department of Health and Human Services, National Institutes of Health, National Cancer Institute (NCI). 2011-02-02.
- PMID 33161240.