Table 15.

Details of different anti-HER2 ADCs in development

ADC name	Antibody	Linker	Toxin	Key IP right	Company	Status	Claim language
Trastuzumab emtansine	Trastuzumab	SMCC	DM1	US8337856	Genentech	Approved in US and EU	An immunoconjugate comprising an anti-ErbB2 antibody conjugated to a maytansinoid, wherein the antibody is huMAb4D5–8.
MM-302	scFv anti-HER2	PEG-DSPE	Liposome-encapsulateddoxorubicin	US2014023698	Merrimack	Phase 2/3	A method of treating a human cancer patient by administration of anthracycline - comprising anti-HER2 immunoliposomes, the method comprising determining a first dosage, such a dosage indicating a dose magnitude and frequency of dosing, for a patient diagnosed with a cancer characterized by expression of HER2 receptor, the first dosage being for a liposomal anthracycline chemotherapeutic agent that does not comprise an immunoliposome, which dosage is determined to provide to the patient a safe and effective amount of the liposomal formulation, and administering anthracycline-comprising anti-HER2 immunoliposomes, a plurality of which immunoliposomes is each bearing a plurality of anti-HER2 antibody molecules on its surface and each containing the anthracycline chemotherapeutic agent, wherein the anthracycline-comprising anti-HER2 immunoliposomes are administered to the patient at the first dosage.
SYD985	Trastuzumab	SpaceLink	Duocarmycin	EP2560645A2	Syntarga	Phase 1	A compound of formula (III): or a pharmaceutically acceptable salt, hydrate, or solvate thereof, wherein […]
ARX788	Undisclosed	Undisclosed	Amberstatin AS269	US2015141624	AmbrX	Preclinical*	wherein […]
Not available	Trastuzumab	Transglutaminase + EENC linker	MMAE, hybrid ADCs with different toxins	Not available	Dophen	R&D	Not available
Not available	Trastuzumab	SMAC with N-terminal LPTXG tag/linker	(i) DM1 (mertansine), (ii) maytansine, (iii) MMAE/MMAF (iv) α-amanitin (v) undisclosed new toxin, respectively	(i) – (iv) WO2014140317 (v) not disclosed	NBE Therapeutics	R&D	1. A method of producing an immunoligand/payload conjugate, which method encompasses conjugating a payload to an immunoligand by means of a sequence- specific transpeptidase, or a catalytic domain thereof. 6. The method according to any of the aforementioned claims, wherein the sequence-specific transpepeptidase is at least one selected from the group consisting of• a sortase enzyme, or one or more fragments or derivatives thereof• a split-intein, or one or more fragments or derivatives thereof
Not available	Trastuzumab	N-Hydroxysuccinimide ester	Tubulysin	Not available	VUMC Amsterdam	R&D	Not available

^*Phase 1 study (NCT02512237) scheduled to start in September 2015; the symbol […] indicates that claim language has been truncated.