IC50: 2.5 ng/mL (CD30)[2]
Brentuximab vedotin (cAC10-vcMMAE) is an antibody-drug conjugate (ADC) comprising an anti-CD30 antibody and the cytotoxic agent Monomethyl auristatin E (MMAE). Brentuximab vedotin inhibits CD30-positive cells with an IC50 of 2.5 ng/mL. Brentuximab vedotin can be used for the research of relapsed and refractory Hodgkin lymphoma[1][2].
Brentuximab vedotin (cAC10-vcMMAE) (1 μg/mL; 96 h) shows cytotoxicity to CD30+ in Karpas 299 cells[2].
Brentuximab vedotin (CAC10-VCMMAE) (1 μg/mL; 12, 24 and 48 h) selectively induces growth arrest in G2/M phase then lead to apoptotic cell death[2].
Cell Cytotoxicity Assay[2]
| Cell Line: | Karpas 299 cells |
| Concentration: | 1 μg/mL |
| Incubation Time: | 96 h |
| Result: | Showed cytotoxicity to CD30+ Karpas 299 cells with an IC50 value of 2.5 ng/mL. |
Cell Cycle Analysis[2]
| Cell Line: | L540 cells |
| Concentration: | 1 μg/mL |
| Incubation Time: | 12, 24, and 48 h |
| Result: | Selectively induced growth arrest in G2/M phase to apoptotic cell death. |
Brentuximab vedotin (cAC10-vcMMAE) (10-120 mg/kg; i.p. for 3 weeks) the maximum tolerated dose (MTD) is between 30 and 40 mg/kg[2].
Brentuximab vedotin (cAC10-vcMMAE) (0.3, 1 mg/kg; flanks injection; every 4 days for a total of 4 doses 1 mg/kg) induces tumor CD30 regression[2].
| Animal Model: | SCID mice[2] |
| Dosage: | 10 to 120 mg/kg |
| Administration: | Intravenous injection; 10 to 120 mg/kg; for 3 weeks |
| Result: | Showed an maximum tolerated dose between 30 and 40 mg/kg. |
| Animal Model: | SCID mice[2] |
| Dosage: | 0.3 and 1 mg/kg |
| Administration: | Flanks injection; 1 mg/kg every 4 days for a total of 4 doses; 0.3 mg/kg every 4 days for a total of 4 doses |
| Result: | Induced complete and durable tumor regression, but 0.3 mg/kg provided lower therapy than 1 mg/kg dose. |
[1]. Shea L, Mehta-Shah N. Brentuximab Vedotin in the Treatment of Peripheral T Cell Lymphoma and Cutaneous T Cell Lymphoma. Curr Hematol Malig Rep. 2020 Feb;15(1):9-19.
[2]. Francisco JA, et al. cAC10-vcMMAE, an anti-CD30-monomethyl auristatin E conjugate with potent and selective antitumor activity. Blood. 2003 Aug 15;102(4):1458-65.