Clinical Development Consultant, Melbourne Beach, FL, USA.
Clinical Development Consultant, Rolesville, NC, USA.
Vascul Pharmacol. 2021 Jun;138:106840. doi: 10.1016/j.vph.2021.106840. Epub 2021 Feb 2.
Treprostinil is a synthetic prostacyclin analogue approved for inhalation administration to patients with pulmonary arterial hypertension (PAH) via nebulized Tyvaso® inhalation solution. LIQ861 is an inhaled, dry-powder formulation of treprostinil produced using Print® (Particle Replication in Nonwetting Templates) technology, a proprietary process for designing and producing highly uniform drug particles.
We conducted comparative bioavailability analyses of treprostinil exposure from LIQ861 (79.5 μg capsule [approximate delivered dose of 58.1 μg treprostinil]) compared with Tyvaso® (9 breaths [approximate delivered dose of 54 μg treprostinil]).
Treprostinil exposure parameters had least squares geometric mean ratios (LIQ861: Tyvaso®) between 0.9 and 1.0 with 90% confidence intervals contained within 0.8 to 1.25. LIQ861 and Tyvaso® were both well tolerated.
Results showed comparable bioavailability of treprostinil and similar tolerability for LIQ861 and Tyvaso® administered to healthy adults.
Given the comparable treprostinil bioavailability and similar safety profiles of LIQ861 and Tyvaso®, LIQ861 fulfills a significant unmet need for PAH patients by maximizing the therapeutic benefits of treprostinil by safely delivering doses to the lungs in 1 to 2 breaths using a discreet, convenient, easy-to-use inhaler.
曲前列尼尔是一种合成前列环素类似物，已被批准通过雾化 Tyvaso®吸入溶液用于治疗肺动脉高压（PAH）患者。LIQ861 是一种使用 Print®（非湿模板中的粒子复制）技术制成的曲前列尼尔干粉吸入制剂，这是一种专有的设计和生产高度均匀药物颗粒的工艺。
我们对 LIQ861（79.5μg 胶囊[约 58.1μg 曲前列尼尔的实际给药剂量]）与 Tyvaso®（9 次呼吸[约 54μg 曲前列尼尔的实际给药剂量]）的曲前列尼尔暴露进行了比较生物利用度分析。
曲前列尼尔暴露参数的最小二乘几何均数比值（LIQ861：Tyvaso®）在 0.9 到 1.0 之间，90%置信区间在 0.8 到 1.25 之间。LIQ861 和 Tyvaso®均具有良好的耐受性。
结果表明，LIQ861 和 Tyvaso®在健康成年人中具有相似的曲前列尼尔生物利用度和相似的耐受性。
鉴于 LIQ861 和 Tyvaso®具有相似的曲前列尼尔生物利用度和安全性特征，LIQ861 通过使用一种 discreet、方便、易于使用的吸入器在 1 到 2 次呼吸内将剂量安全地输送到肺部，最大限度地提高了曲前列尼尔的治疗效益，满足了 PAH 患者的重大未满足需求。
