A Randomized, Open-Label, Single-Dose, Parallel-Group Study to Evaluate the Relative Bioavailability of LY03010 versus Xeplion® after Intramuscular Injection in Healthy Subjects

Trial details

Who runs it

Geneora Pharma (Shijiazhuang) Co. Ltd.

Trial code

EU 2022-502179-48-00

Record updated

2024. február 28.

Original description

To evaluate the relative bioavailability of paliperidone in LY03010 versus in Xeplion® following a single-dose IM injection in healthy subjects.Read full original descriptionShow less

To evaluate the relative bioavailability of paliperidone in LY03010 versus in Xeplion® following a single-dose IM injection in healthy subjects.

Inclusion: Willing and capable of giving informed consent; Willing and able to comply with study procedures, adhere to study restrictions, and stay at the clinical research unit during in-subject stays required by the protocol; Male or female ≥18 to ≤55 years of age, inclusive; Healthy, per investigator’s judgment, based on detailed medical history, clinical laboratory safety tests, vital signs, full physical examination, and ECGs; Body mass index (BMI) between 18.5 and 30 kg/m2, inclusive; body weight ≥50 kg at screening; Prolactin laboratory value within normal range; All female subjects must have negative pregnancy test results at screening. Female subjects must meet 1 of the following 3 conditions: (i) postmenopausal for at least 12 months without an alternative medical cause, (ii) surgically sterile (hysterectomy, bilateral oophorectomy, bilateral salpingectomy, or bilateral tubal occlusion) based on subject report, or (iii) if of childbearing potential and heterosexually active, practicing or agreeing to practice a highly effective contraception method of birth control. Highly effective methods of birth control include an intrauterine device (IUD), intrauterine hormone-releasing system (IUS), and contraceptives (oral, skin patches, or implanted or injectable products) using combined or progestogen-only hormonal contraception associated with inhibition of ovulation. A vasectomized male partner is an acceptable birth control method if the vasectomized partner is the sole sexual partner of the female subject and the vasectomized partner has received medical confirmation of surgical success. Highly effective methods of birth control must be used for at least 21 days prior to first Risperdal® administration, throughout the study until the end-of-study (EOS) visit (or at least 148 days after the dose, whichever is longer) to minimize the risk of pregnancy; Sexually active fertile male subjects must be willing to use acceptable contraception methods (condom) from first Risperdal® administration , throughout the study until the EOS visit (or at least 148 days after the dose, whichever is longer) if their partners are women of childbearing potential.

Exclusion: Subjects who have received COVID-19 vaccines within the last 14 days prior to baseline or plan to get vaccinated within 30 days after dosing; Hospital admission or major surgery within 30 days prior to screening; Receipt of another investigational product within 1 month, or 5 half-lives of the other investigational product, whichever is longer, prior to screening; Donation or blood collection of > 1 unit (approximate 450 mL) of blood (or blood products) or acute loss of blood during the 90 days prior to screening; History of prescription drug or alcohol abuse, or any illicit drug use within 6 months prior to screening or at baseline; Positive screen for alcohol and illicit drugs at screening; Use of prescription or over-the-counter (OTC) medications and/or herbal supplements (including St John’s Wort, herbal) within 14 days prior to dosing; Intake of grapefruit/grapefruit juice within 7 days prior to dosing; Consumption of any alcoholic product within the previous 24 hours; Positive result in urine drugs-of-abuse test or ethanol urine test; Malignancies within 5 years with the exception of cured basal cell or squamous cell skin cancer or in situ cervical cancer prior to screening; Clinically significant past medical history of gastrointestinal, cardiovascular, cerebrovascular, musculoskeletal, endocrine, hematologic, renal, hepatic, bronchopulmonary, neurologic, immunologic disorders, and/or drug hypersensitivity which, in the judgement of the Investigator, would interfere with the subject’s ability to participate in the study; Negative SARS-CoV-2 test or valid EU Digital COVID-19 Recovery Certificate; Subject who had severe course of COVID-19 (i.e., hospitalization, extracorporeal membrane oxygenation (ECMO), and/or mechanically ventilated); Subjects who show an allergic reaction to risperidone tolerability test will be excluded from the study; History of epilepsy or convulsive disorder other than a single childhood febrile seizure; Any recent disease or condition or treatment that, according to the Investigator, would put the subject at undue risk due to study participation or occurred at a timeframe in which may interfere with the pharmacokinetics of study drug; History of Parkinson’s diseases, Dementia with Lewy Bodies or Dementia-related psychosis; Any other condition that, according to the Investigator, renders the subject unsuitable for the study; History of neuroleptic malignant syndrome (NMS) or tardive dyskinesia of any cause; History of symptomatic orthostatic hypotension, or currently with a decrease of ≥20 mmHg in systolic blood pressure (SBP) or decrease of ≥10 mmHg in diastolic blood pressure (DBP) when changing from supine to standing position after having been in the supine position for at least 5 minutes or SBP less than 105 mmHg in supine position at screening; Positive blood screen for human immunodeficiency virus (HIV) antibody, hepatitis B surface antigen (HBsAg), or hepatitis C antibody at screening; Hemoglobin A1c (HbAlc) level ≥5.7% at screening; White blood cells <3×109/L, or neutrophils outside the limit of normal range; Any clinical observation or clinical laboratory abnormality findings at screening or baseline visits which, in the opinion of the Investigator, may endanger the subject or interfere with the endpoints of the study. If the results of clinical laboratory testing are outside normal reference ranges, the subject may be enrolled but only if these findings are determined not to be clinically significant by the Investigator; Indication of impaired renal function at Screening (estimated glomerular filtration rate < 90 mL/min); Positive pregnancy test result or plan to become pregnant within the study duration, if female; Female who is pregnant or breastfeeding or of childbearing potential without adequate contraception (see Inclusion Criterion #7); If female of childbearing potential, positive pregnancy test in urine; Subjects who pose a significant risk of a suicide attempt based on history or the Investigator’s judgment; answer “yes” to Suicidal Ideation items 4 or 5 on the Columbia Suicide Severity Rating Scale (C-SSRS) for current or past 3 months on the “Baseline/Screening version” at screening; have had suicidal behavior in his/her lifetime as measured by the C-SSRS at screening; or are at imminent risk of suicide or violent behavior based on the Investigator’s clinical assessment or the C-SSRS assessment of lifetime suicidal ideation or behavior at screening; QTcF interval greater than 450 msec for males and 460 msec for females at screening, or other clinically significant ECG findings in the opinion of the Investigator.

EU CTIS 2022-502179-48-00