A Study Assessing the Safety and Tolerability of LY03020 in Chinese Healthy Subjects

The study will set 2.5mg, 5mg, 10mg, 20mg, 40mg, 60mg, 80mg and 100mg, a total of 8 dose groups. Qualified subjects were enrolled in site at D-1 ( 1 day before administration ) and randomized.The subjects should fast for at least 10 hours before medication administration, with no restrictions on water intake. The subjects will be required to orally take LY03020 or a placebo on an empty stomach upon waking on D1 (the day of medication administration). From D1 to D7, they will undergo safety assessments and PK biological sample collection.

• LY03020 (Drug), also known as LPM787000048 Maleate sustained-release tablet: LY03020 for one single dose
• Placebo (Drug), also known as Placebo of LPM787000048 Maleate sustained-release tablet: Placebo for one single dose

Primary outcomes

• Frequency of adverse events (AEs) [up to144 hours]: Percentage of adverse events

Secondary outcomes

• Maximum observed concentration (Cmax) of LPM787000048 in plasma [up to144 hours]: Subject blood samples will be collected at 17 time points and pharmacokinetic parameters will be calculated.
• Time to maximum observed concentration (Tmax) of LPM787000048 in plasma [up to144 hours]: Subject blood samples will be collected at 17 time points and pharmacokinetic parameters will be calculated.
• Area under the concentration-time curve from time zero extrapolated to infinity (AUC0-∞) of LPM787000048 in plasma [up to144 hours]: Subject blood samples will be collected at 17 time points and pharmacokinetic parameters will be calculated.
• Area under the concentration-time curve from time zero to the time of last quantifiable concentration (AUC0-t) of LPM787000048 in plasma [up to144 hours]: Subject blood samples will be collected at 17 time points and pharmacokinetic parameters will be calculated.
• Apparent terminal elimination half-life (t1/2) of LPM787000048 in plasma [up to144 hours]: Subject blood samples will be collected at 17 time points and pharmacokinetic parameters will be calculated.
• Apparent volume of distribution（Vz/F） of LPM787000048 in plasma [up to144 hours]: Subject blood samples will be collected at 17 time points and pharmacokinetic parameters will be calculated.
• Apparent total body clearance (CL/F) of LPM787000048 from plasma [up to144 hours]: Subject blood samples will be collected at 17 time points and pharmacokinetic parameters will be calculated.

Other outcomes

• Quantitatively determine the concentration of LPM787000048 and major metabolites (if applicable) in urine and calculate the cumulative excretion ratio in urine. [up to144 hours]: One dose group will be selected for metabolite identification.

Sex: All, ages: 18 Years to 45 Years, accepts healthy volunteers

Inclusion Criteria:

* Subjects sign informed consent voluntarily.
* Male or female aged 18 to 45 years.
* Body weight ≥ 50.0 kg for male and ≥ 45.0 kg for female, and male or female greater than or equal to 18.5 but less than 26.0 kg/m2 of body mass index (BMI).

Exclusion Criteria:

* Subjects have any clinically significant medical condition or chronic disease.
* Subjects experienced a history of keratopathy, fundus disease, increased intraocular pressure,or angle-closure glaucoma.Subjects have a abnormal and clinically significant test for ophthalmic examination during screening.
* Subjects with condition that may interfere with the drug absorption, distribution, metabolism and excretion significantly.
* Subjects had a history of surgery within 3 months prior to administration, or had not recovered, or have a surgical plan during the study.
* Subjects have any clinically significant abnormal vital signs, laboratory values, and ECGs.
* Subjects have used any of nonprescription drugs within 7 days or prescription drugs within 28 days prior to administration.
* Subjects have a history of allergic diseases, or allergic to any substance contained in the formulation
* Subjects have a positive test for HBsAg, HCV-Ab, HIV-Ab, or syphilis serum reaction.

• Gang Wang, Principal investigator, Beijing AnDing Hospital Capital Medical University