To evaluate the safety, tolerability, dose limiting toxicity (DLT), and maximum tolerated dose (MTD), of FS102(BMS-986186) when administered intravenously (IV) to subjects with relapsed or refractory solid tumors that overexpress HER2 and who have no standard treatment options.

Start Date04 Nov 2014

Sponsor / Collaborator

Bristol Myers Squibb Co.

100 Clinical Results associated with BMS-986186

100 Translational Medicine associated with BMS-986186

100 Patents (Medical) associated with BMS-986186

Literatures (Medical) associated with BMS-986186

01 Nov 2015·Molecular TherapyQ1 · MEDICINE

A HER2-specific Modified Fc Fragment (Fcab) Induces Antitumor Effects Through Degradation of HER2 and Apoptosis

Q1 · MEDICINE

Article

Author: Isaac, Samine J ; Wydro, Mateusz M ; Gaspar, Miguel ; Haurum, John S ; Moulder, Kevin ; Carvalho, Joana ; Batey, Sarah ; Weller, Sarah ; Medcalf, Melanie ; Pegram, Robert ; Sun, Haijun ; Mudde, Geert C ; Rowlands, Robert ; Drewett, Victoria ; Woisetschläger, Max ; Jones, Phil ; Bauer, Anton ; Tuna, Mihriban ; Leung, Kin-Mei

FS102 is a HER2-specific Fcab (Fc fragment with antigen binding), which binds HER2 with high affinity and recognizes an epitope that does not overlap with those of trastuzumab or pertuzumab. In tumor cells that express high levels of HER2, FS102 caused profound HER2 internalization and degradation leading to tumor cell apoptosis. The antitumor effect of FS102 in patient-derived xenografts (PDXs) correlated strongly with the HER2 amplification status of the tumors. Superior activity of FS102 over trastuzumab or the combination of trastuzumab and pertuzumab was observed in vitro and in vivo when the gene copy number of HER2 was equal to or exceeded 10 per cell based on quantitative polymerase chain reaction (qPCR). Thus, FS102 induced complete and sustained tumor regression in a significant proportion of HER2-high PDX tumor models. We hypothesize that the unique structure and/or epitope of FS102 enables the Fcab to internalize and degrade cell surface HER2 more efficiently than standard of care antibodies. In turn, increased depletion of HER2 commits the cells to apoptosis as a result of oncogene shock. FS102 has the potential of a biomarker-driven therapeutic that derives superior antitumor effects from a unique mechanism-of-action in tumor cells which are oncogenically addicted to the HER2 pathway due to overexpression.

100 Deals associated with BMS-986186

R&D Status

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Indication	Highest Phase	Country/Location	Organization	Date
Breast Cancer	Phase 1	-	F Star Co., Ltd.	-
Breast Cancer	Phase 1	-	Bristol Myers Squibb Co.	-
Stomach Cancer	Phase 1	-	Bristol Myers Squibb Co.	-
Stomach Cancer	Phase 1	-	F Star Co., Ltd.	-
HER2 Positive Solid Tumors	Preclinical	US	Bristol Myers Squibb Co.	04 Nov 2014
HER2 Positive Solid Tumors	Preclinical	CA	Bristol Myers Squibb Co.	04 Nov 2014

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