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Study terminated by sponsor due a business decision and development strategy.
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| Name | Class |
|---|---|
| Asieris Pharmaceuticals (AUS) Pty Ltd. | INDUSTRY |
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The primary objective of the study is to assess safety and tolerability following administration of single doses of APL-1202 (immediate release) IR tablets and APL-1501 extended release (ER) capsules in healthy participants.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Cohort 1, Sequence 1, R1T1: APL-1202 IR 375 mg + APL-1501 ER 764 mg | Experimental | Participants will receive APL-1202 375 milligram (mg) IR tablets, orally, once on Day 1 of Period 1 (Treatment R1), followed by T1 APL-1501 764 mg ER capsules, orally, once, on Day 4 of Period 2 (Treatment T1). A washout period of more than or equal to (>=) 72 hours will be maintained in between Period 1 and 2. |
|
| Cohort 1, Sequence 2, T1R1: APL-1501 ER 764 mg + APL-1202 IR 375 mg | Experimental | Participants will receive APL-1501 764 mg ER capsules, orally, once on Day 1 of Period 1 (Treatment T1), followed by APL-1202 375 mg IR tablets, orally, once, on Day 4 of Period 2 (Treatment R1). A washout period of >=72 hours will be maintained in between Period 1 and 2. |
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| Cohort 2, Sequence 1, R1T2: APL-1202 IR 375 mg + APL-1501 ER 1146 mg | Experimental | Participants will receive APL-1202 375 mg IR tablets, orally, once on Day 1 of Period 1 (Treatment R1), followed by APL-1501 1146 mg ER capsules, orally, once, on Day 4 of Period 2 (Treatment T2). A washout period of >=72 hours will be maintained in between Period 1 and 2. |
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| Cohort 2, Sequence 2, T2R1: APL-1501 ER 1146 mg + APL-1202 IR 375 mg | Experimental | Participants will receive APL-1501 1146 mg ER capsules, orally, once on Day 1 of Period 1 (Treatment T2), followed by APL-1202 375 mg IR tablets, orally, once, on Day 4 of Period 2 (Treatment R1). A washout period of >=72 hours will be maintained in between Period 1 and 2. |
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| APL-1202 | Drug | APL-1202 IR tablets. |
|
| Measure | Description | Time Frame |
|---|---|---|
| Number of Participants With Adverse Events (AEs) | From Baseline up to Day 9 | |
| Number of Participants With Abnormal Vital Sign Measurements | From Baseline up to Day 9 | |
| Number of Participants With Abnormal 12-Lead Electrocardiogram (ECGs) Recordings | From Baseline up to Day 9 | |
| Number of Participants With Abnormal Physical Examinations | From Baseline up to Day 9 | |
| Number of Participants With Abnormal Clinical Laboratory Values | From Baseline up to Day 9 |
| Measure | Description | Time Frame |
|---|---|---|
| AUC0-t: Area Under the Concentration-time Curve From Time Zero Until the Last Observed Concentration of APL-1202, and ASN-1651 (Metabolite) Following APL-1501 ER Capsules | Cohorts 1 and 2 - Days 1 and 4: Pre-dose and up to 24 hours post-dose; Cohort 3 - Day 1: Pre-dose and up to 24 hours post-dose | |
| AUC0-inf: Area Under the Concentration-time Curve From Time Zero to Infinity of APL-1202, and ASN-1651 (Metabolite) Following APL-1501 ER Capsules |
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Inclusion Criteria:
Participants must meet all of the following criteria to be included in the study:
Male, >=18 and less than or equal to (<=) 65 years of age, with body mass index (BMI) greater than (>) 18.5 and less than (<) 32.0 kilogram per square meter (kg/m^2) and body weight >=50.0 kilogram (kg).
Non-smoker (no use of tobacco or nicotine products, example, snuff, chewing tobacco, cigars, cigarettes, pipes, e-cigarettes [vaping] etc. within 3 months prior to screening).
Healthy as defined by:
Sexually active non-sterile males must be willing to use an acceptable contraceptive method throughout the study.
Able to understand the study procedures and provide signed informed consent to participate in the study.
Exclusion Criteria:
Participants to whom any of the following applies will be excluded from the study:
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| Name | Affiliation | Role |
|---|---|---|
| Dr Christopher Argent | Asieris Pharmaceuticals (AUS) Pty Ltd. | Principal Investigator |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Scientia Clinical Research Ltd | Randwick | New South Wales | 2031 | Australia |
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| ID | Term |
|---|---|
| D001749 | Urinary Bladder Neoplasms |
| ID | Term |
|---|---|
| D014571 | Urologic Neoplasms |
| D014565 | Urogenital Neoplasms |
| D009371 | Neoplasms by Site |
| D009369 | Neoplasms |
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| Cohort 3: APL-1501 ER 1528 mg | Experimental | Participants will receive APL-1501 1528 mg ER capsules, orally, once on Day 1. |
|
| APL-1501 | Drug | APL-1501 ER capsules. |
|
| Cohorts 1 and 2 - Days 1 and 4: Pre-dose and up to 24 hours post-dose; Cohort 3 - Day 1: Pre-dose and up to 24 hours post-dose |
| Cmax: Maximal Observed Concentration of APL-1202, and ASN-1651 (Metabolite) Following APL-1501 ER Capsules | Cohorts 1 and 2 - Days 1 and 4: Pre-dose and up to 24 hours post-dose; Cohort 3 - Day 1: Pre-dose and up to 24 hours post-dose |
| Tlast: Time When the Last Concentration is Observed of APL-1202, and ASN-1651 (Metabolite) Following APL-1501 ER Capsules | Cohorts 1 and 2 - Days 1 and 4: Pre-dose and up to 24 hours post-dose; Cohort 3 - Day 1: Pre-dose and up to 24 hours post-dose |
| Tmax: Time When the Cmax is Observed of APL-1202, and ASN-1651 (Metabolite) Following APL-1501 ER Capsules | Cohorts 1 and 2 - Days 1 and 4: Pre-dose and up to 24 hours post-dose; Cohort 3 - Day 1: Pre-dose and up to 24 hours post-dose |
| Residual Area of APL-1202, and ASN-1651 (Metabolite) Following APL-1501 ER Capsules | Residual area is defined as percentage of AUC0-inf due to extrapolation from the time of the last observed concentration to infinity and is calculated as, [1-(AUC0-t/AUC0-inf)]*100. | Cohorts 1 and 2 - Days 1 and 4: Pre-dose and up to 24 hours post-dose; Cohort 3 - Day 1: Pre-dose and up to 24 hours post-dose |
| T½ el: Terminal Elimination Half-life of APL-1202, and ASN-1651 (Metabolite) Following APL-1501 ER Capsules | Cohorts 1 and 2 - Days 1 and 4: Pre-dose and up to 24 hours post-dose; Cohort 3 - Day 1: Pre-dose and up to 24 hours post-dose |
| Kel: Terminal Elimination Rate Constant of APL-1202, and ASN-1651 (Metabolite) Following APL-1501 ER Capsules | Cohorts 1 and 2 - Days 1 and 4: Pre-dose and up to 24 hours post-dose; Cohort 3 - Day 1: Pre-dose and up to 24 hours post-dose |
| Cl/F: Apparent Clearance of APL-1202, and ASN-1651 (Metabolite) Following APL-1501 ER Capsules | Cohorts 1 and 2 - Days 1 and 4: Pre-dose and up to 24 hours post-dose; Cohort 3 - Day 1: Pre-dose and up to 24 hours post-dose |
| Vz/F: Apparent Volume of Distribution of APL-1202, and ASN-1651 (Metabolite) Following APL-1501 ER Capsules | Cohorts 1 and 2 - Days 1 and 4: Pre-dose and up to 24 hours post-dose; Cohort 3 - Day 1: Pre-dose and up to 24 hours post-dose |
| DNAUC0-inf: Dose Normalized AUC0-inf of APL-1202, and ASN-1651 (Metabolite) Following APL-1501 ER Capsules | Cohorts 1 and 2 - Days 1 and 4: Pre-dose and up to 24 hours post-dose; Cohort 3 - Day 1: Pre-dose and up to 24 hours post-dose |
| DNCmax: Dose Normalized Cmax of APL-1202, and ASN-1651 (Metabolite) Following APL-1501 ER Capsules | Cohorts 1 and 2 - Days 1 and 4: Pre-dose and up to 24 hours post-dose; Cohort 3 - Day 1: Pre-dose and up to 24 hours post-dose |
| Geometric Mean Ratio of Cmax of APL-1501 ER Capsules in Reference to APL-1202 IR Tablets | Cohorts 1 and 2 - Days 1 and 4: Pre-dose and up to 24 hours post-dose; Cohort 3 - Day 1: Pre-dose and up to 24 hours post-dose |
| Geometric Mean Ratio of AUC0-t of APL-1501 ER Capsules in Reference to APL-1202 IR Tablets | Cohorts 1 and 2 - Days 1 and 4: Pre-dose and up to 24 hours post-dose; Cohort 3 - Day 1: Pre-dose and up to 24 hours post-dose |
| Geometric Mean Ratio of AUC0-inf of APL-1501 ER Capsules in Reference to APL-1202 IR Tablets | Cohorts 1 and 2 - Days 1 and 4: Pre-dose and up to 24 hours post-dose; Cohort 3 - Day 1: Pre-dose and up to 24 hours post-dose |
| Frel: Relative Bioavailability of APL-1501 ER Capsules and APL-1202 IR Tablets | The relative bioavailability of APL-1501 versus APL-1202 will be assessed through linear mixed modelling. | Cohorts 1 and 2 - Days 1 and 4: Pre-dose and up to 24 hours post-dose; Cohort 3 - Day 1: Pre-dose and up to 24 hours post-dose |
| Dose Proportionality of Cmax | Dose proportionality will be assessed by visual inspection of dose normalised Cmax values versus dose. | Cohorts 1 and 2 - Days 1 and 4: Pre-dose and up to 24 hours post-dose; Cohort 3 - Day 1: Pre-dose and up to 24 hours post-dose |
| Dose Proportionality of AUC0-t | Dose proportionality will be assessed by visual inspection of dose normalised AUC0-t values versus dose. | Cohorts 1 and 2 - Days 1 and 4: Pre-dose and up to 24 hours post-dose; Cohort 3 - Day 1: Pre-dose and up to 24 hours post-dose |
| Dose Proportionality of AUC0-inf | Dose proportionality will be assessed by visual inspection of dose normalised AUC0-inf values versus dose. | Cohorts 1 and 2 - Days 1 and 4: Pre-dose and up to 24 hours post-dose; Cohort 3 - Day 1: Pre-dose and up to 24 hours post-dose |
| D052776 |
| Female Urogenital Diseases |
| D005261 | Female Urogenital Diseases and Pregnancy Complications |
| D000091642 | Urogenital Diseases |
| D001745 | Urinary Bladder Diseases |
| D014570 | Urologic Diseases |
| D052801 | Male Urogenital Diseases |