Decibel Therapeutics, 1325 Boylston Street, Suite 500, Boston, MA, 02215, USA.
Invest New Drugs. 2020 Oct;38(5):1463-1471. doi: 10.1007/s10637-020-00918-1. Epub 2020 Mar 10.
Cisplatin is a widely used chemotherapy for the treatment of certain solid tumors. Ototoxicity and subsequent permanent hearing loss remain a serious dose-limiting side effect associated with cisplatin treatment. To date, no therapies have been approved to prevent or treat cisplatin-induced hearing loss (CIHL). Sodium thiosulfate effectively inactivates cisplatin through covalent binding and may provide protection against cisplatin-induced ototoxicity. DB-020 is being developed as a novel formulation of sodium thiosulfate pentahydrate in 1% sodium hyaluronate for intratympanic injection (IT), enabling the delivery of high concentrations of thiosulfate into the cochlea prior to cisplatin administration. In the DB-020-002 phase 1a single-ascending dose study, healthy volunteers were enrolled into 5 cohorts to receive different doses of DB-020 via IT injection. Cohorts 1-4 received unilateral injections while Cohort 5 received bilateral injections. Plasma thiosulfate pharmacokinetics was measured, and safety and audiometric data were collected throughout the study. This study has demonstrated that intratympanic administration of DB-020 results in nominal systemic increases in thiosulfate levels, hence it should not compromise cisplatin anti-tumor efficacy. Furthermore, DB-020 was safe and well tolerated with most adverse events reported as transient, of mild-to-moderate severity and related to the IT administration procedure. These results support the design and execution of the ongoing proof-of-concept study, DB-020-002, to assess otoprotection using DB-020 in cancer patients receiving cisplatin without negatively impacting cisplatin anti-tumor efficacy.
顺铂是一种广泛用于治疗某些实体瘤的化疗药物。耳毒性和随后的永久性听力损失仍然是与顺铂治疗相关的严重剂量限制的副作用。迄今为止,尚无批准的疗法可预防或治疗顺铂引起的听力损失(CIHL)。硫代硫酸钠通过共价键有效地使顺铂失活,可能提供针对顺铂诱导的耳毒性的保护。DB-020 正在开发为 1%透明质酸钠中五水合硫代硫酸钠的新型制剂,用于鼓室内注射(IT),使顺铂给药前可将高浓度的硫代硫酸盐递送至耳蜗。在 DB-020-002 期 1a 单上升剂量研究中,健康志愿者被招募到 5 个队列中,通过 IT 注射接受不同剂量的 DB-020。队列 1-4 接受单侧注射,而队列 5 接受双侧注射。测量了血浆硫代硫酸盐药代动力学,并在整个研究过程中收集了安全性和听力数据。这项研究表明,鼓室内给予 DB-020 可使硫代硫酸盐水平名义上增加,因此不会影响顺铂的抗肿瘤疗效。此外,DB-020 是安全且耐受良好的,大多数不良反应报告为短暂的、轻度至中度严重程度,且与 IT 给药程序有关。这些结果支持正在进行的概念验证研究 DB-020-002 的设计和执行,以使用 DB-020 评估接受顺铂治疗的癌症患者的耳保护作用,而不会对顺铂的抗肿瘤疗效产生负面影响。