Erzotabart is an IgG1-kappa, anti- CD38 (ADP-ribosyl cyclase 1, cyclic ADP-ribose hydrolase 1, cADPr hydrolase 1, cADPR1) Homo sapiens monoclonal antibody. Erzotabart shows antineoplastic activity [1].
In Vivo, Erzotabart (10 mg/kg, iv, once weekly for 3 weeks) exhibits antitumor activity against B-cell non-Hodgkin lymphoma (B-NHL) and acute myeloid leukaemia (AML) in mouse models[3].
In Vitro, Erzotabart targets cell surface glycoprotein CD-38 and carries the E430G mutation. Erzotabart promotes antibody hexamer formation through the E430G mutation in the Fc segment, and exhibits immunomodulating and antineoplastic activities[2]. Erzotabart induces complement-dependent cytotoxicity (CDC), antibody-dependent cellular cytotoxicity (ADCC), antibody-dependent cellular phagocytosis (ADCP), trogocytosis, inhibits the cyclase activity of CD38, and increases the hydrolase activity with EC50s of 0.044 µg/mL, 0.29 ng/mL, 2.719-5.779 ng/mL, 8.79 ng/mL, 0.419 µg/mL and 0.335 µg/mL, respectively[3].
References:
[1]. International Nonproprietary Names for Pharmaceutical Substances (INN). WHO Drug Information, Vol. 36, No. 4, 2022.
[2]. Grosicki S, et al. GEN3014 (HexaBody®-CD38) in anti-CD38 Mab-naive patients with relapsed/refractory multiple myeloma: preliminary results from a dose-expansion cohort of a phase 1/2 trial[J]. Blood, 2023, 142: 4757.
[3]. Hiemstra IH, et al., Preclinical anti-tumour activity of HexaBody-CD38, a next-generation CD38 antibody with superior complement-dependent cytotoxic activity. EBioMedicine. 2023 Jul;93:104663.
In Vivo, Erzotabart (10 mg/kg, iv, once weekly for 3 weeks) exhibits antitumor activity against B-cell non-Hodgkin lymphoma (B-NHL) and acute myeloid leukaemia (AML) in mouse models[3].
In Vitro, Erzotabart targets cell surface glycoprotein CD-38 and carries the E430G mutation. Erzotabart promotes antibody hexamer formation through the E430G mutation in the Fc segment, and exhibits immunomodulating and antineoplastic activities[2]. Erzotabart induces complement-dependent cytotoxicity (CDC), antibody-dependent cellular cytotoxicity (ADCC), antibody-dependent cellular phagocytosis (ADCP), trogocytosis, inhibits the cyclase activity of CD38, and increases the hydrolase activity with EC50s of 0.044 µg/mL, 0.29 ng/mL, 2.719-5.779 ng/mL, 8.79 ng/mL, 0.419 µg/mL and 0.335 µg/mL, respectively[3].
References:
[1]. International Nonproprietary Names for Pharmaceutical Substances (INN). WHO Drug Information, Vol. 36, No. 4, 2022.
[2]. Grosicki S, et al. GEN3014 (HexaBody®-CD38) in anti-CD38 Mab-naive patients with relapsed/refractory multiple myeloma: preliminary results from a dose-expansion cohort of a phase 1/2 trial[J]. Blood, 2023, 142: 4757.
[3]. Hiemstra IH, et al., Preclinical anti-tumour activity of HexaBody-CD38, a next-generation CD38 antibody with superior complement-dependent cytotoxic activity. EBioMedicine. 2023 Jul;93:104663.