Rovalpituzumab tesirine  (Synonyms: SC-002)

Rovalpituzumab tesirine (SC-002) is an antibody-drug conjugate (ADC) with anticancer effects. Rovalpituzumab tesirine contains a DLL3-targeting antibody Rovalpituzumab (HY-P99043) tethered to a cytotoxic agent pyrrolobenzodiazepine by means of a protease-cleavable linker. Rovalpituzumab tesirine can be used for the stduy of small cell lung cancer (SCLC)^[1].

Rovalpituzumab tesirine (0.01-10000 pM, 96 h) 在表达小鼠 DLL3 的 KP1 细胞 (SCLC 模型) 中，能有效结合小鼠 DLL3 ，表现出强效的杀伤作用，并通过内化 PBD 毒素发挥细胞毒性^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Rovalpituzumab tesirine (0.03, 0.1, 0.3 mg/kg, i.p. one dose) 在 SCLC 小鼠模型中，呈剂量依赖性抑制肿瘤生长，0.3 mg/kg组实现完全缓解，与抗 PD1 联用抗肿瘤效果更加显著^[2]。
Rovalpituzumab tesirine (0.03 mg/kg, i.p once every four days) 在 SCLC 小鼠模型中，与抗 PD1 的联用使得肿瘤内 CD8⁺ T 细胞浸润与活化，上调 PD-L1 和 MHC1，克服免疫抑制，并激活 DC 和 STING 通路，发挥协同抗肿瘤作用^[2]。
Rovalpituzumab tesirine (0.1 mg/kg, i.p. one dose) 在 SCLC 小鼠模型中，与抗 PD1 的联用证实 CD8⁺ T 细胞是疗效的关键效应细胞^[2]。
Rovalpituzumab tesirine (0.03 mg/kg, i.p. one dose) 在 SCLC 小鼠模型中，与抗 PD1 的联用诱导了长期抗肿瘤免疫记忆^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

1613313-09-9

液体

Colorless to light yellow

Shipping with dry ice.

-80°C, protect from light

• [1]. Blackhall F, et al. Efficacy and Safety of Rovalpituzumab Tesirine Compared With Topotecan as Second-Line Therapy in DLL3-High SCLC: Results From the Phase 3 TAHOE Study. J Thorac Oncol. 2021 Sep;16(9):1547-1558.  [Content Brief]

  [2]. Vitorino P, et al. Rova-T enhances the anti-tumor activity of anti-PD1 in a murine model of small cell lung cancer with endogenous Dll3 expression. Transl Oncol. 2021 Jan;14(1):100883.  [Content Brief]