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| ID | Type | Description | Link |
|---|---|---|---|
| 2017-004002-18 | EudraCT Number | ||
| QCL118174 | Other Identifier | Quotient Study Number |
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Part 1 of the study will be conducted to provide additional information on the safety and tolerability of single doses of BOS172767 in healthy participants, to evaluate the pharmacokinetic (PK) profiles (including relative bioavailability) of BOS172767 following oral administration of 3 prototype formulations in healthy participants compared to an immediate release capsule formulation (reference), and also to determine the relative bioavailability of a selected BOS172767 prototype formulation in the fed and fasted states.
Part 2 of the study will be conducted to provide additional information on the safety and tolerability of escalating single doses of the selected formulation of BOS172767 in healthy participants, to evaluate the PK profile following increased single doses of the selected formulation of BOS172767 following administration in healthy participants, and also to evaluate the dose linearity of the selected prototype.
Part 3 of the study will be conducted to provide additional information on the safety, tolerability, and PK of the selected formulation of BOS172767 following multiple ascending doses (MADs) over 14 days of dosing in healthy participants.
Part 1 is comprised of a single-dose, part-randomized, open-label, 6-way crossover in 12 healthy participants. Participants will be dosed on 6 separate occasions (in 6 treatment periods), and will receive a single prototype of BOS172767 in each treatment period.
Part 2 is comprised of a single ascending dose, fixed-sequence, open-label, 3-way crossover with an optional fourth dosing period in 10 healthy participants. Participants will be dosed on 4 separate occasions (in 4 treatment periods), and will receive a single prototype of BOS172767 in each treatment period.
Part 3 is a double-blind (sponsor-open), placebo-controlled, randomized MAD part in 36 healthy participants (12 per study cohort). Participants will be dosed on 3 separate occasions (in 3 treatment periods), and will receive a single prototype of BOS172767 in each treatment period.
Parts 2 and 3 are contingent upon successful completion of Part 1.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Part 1: Regimen A | Experimental | Participants will be treated with a BOS172767 200 milligram (mg) spray dried dispersion tablet (2 × 100 mg tablets) in the fasted state on Day 1. |
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| Part 1: Regimen B | Experimental | Participants will be treated with a BOS172767 200 mg lipid capsule (2 × 100 mg capsules) in the fasted state on Day 1. |
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| Part 1: Regimen C | Experimental | Participants will be treated with a BOS172767 200 mg micronized capsule (2 × 100 mg capsules) in the fasted state on Day 1. |
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| Part 1: Regimen D | Experimental | Participants will be treated with a BOS172767 200 mg immediate release reference capsule formulation (2 × 100 mg capsules) in the fasted state on Day 1. |
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| Part 1: Regimen E | Experimental | Participants will be treated with a selected dose of a prototype formulation of BOS172767 in the fasted state on Day 1. |
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| BOS172767 tablets | Drug | Oral tablets |
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| Measure | Description | Time Frame |
|---|---|---|
| Parts 1, 2, and 3: Number of participants with any treatment-emergent serious adverse event (TESAE) | up to 33 weeks | |
| Parts 1, 2, and 3: Number of participants with any treatment-emergent non-serious adverse event (TEAE) | up to 33 weeks | |
| Parts 1, 2, and 3: Number of participants with abnormal, clinically significant physical examination findings | up to 33 weeks | |
| Parts 1, 2, and 3: Number of participants with abnormal, clinically significant safety laboratory test findings | up to 33 weeks | |
| Parts 1, 2, and 3: Number of participants with abnormal, clinically significant vital sign values | up to 33 weeks | |
| Parts 1, 2, and 3: Number of participants with abnormal, clinically significant electrocardiogram findings | up to 33 weeks | |
| Parts 1 and 2: Plasma concentration of BOS172722 | predose; 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 16 hours postdose (Day 1); 24 and 36 hours postdose (Day 2); 48 hours postdose (Day 3) | |
| Part 2 (Regimen I): Plasma concentration of BOS172722 | admission to pre-dose (admission to dosing), 0 to 6 (Day 1), 6 to 12 (Day 1), 12 to 24 (Day 1), and 24 to 48 (Days 2 to 3) hours postdose | |
| Part 3: Plasma concentration of BOS172722 |
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Inclusion Criteria:
Exclusion Criteria:
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| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Quotient Sciences | Nottingham | United Kingdom |
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Part 1 and 2 of the study are open-label and therefore blinding is not required. Part 3 of the study is double-blind.
| Part 1: Regimen F | Experimental | Participants will be treated with a selected dose of a prototype formulation of BOS172767 in the fed state on Day 1. |
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| Part 2: Regimen G | Experimental | Participants will be treated with 400 mg of the selected BOS172767 prototype in the fasted state on Day 1. |
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| Part 2: Regimen H | Experimental | Participants will be treated with 600 mg of the selected BOS172767 prototype in the fasted state on Day 1. |
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| Part 2: Regimen I | Experimental | Participants will be treated with 800 mg of the selected BOS172767 prototype in the fasted state on Day 1. |
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| Part 2: Regimen J | Experimental | Participants will be treated with rabeprazole on Days -3 to -1, and a selected dose of the BOS172767 prototype in the fasted state on Day 1. |
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| Part 3: Regimen K | Experimental | Participants will be treated with 400 mg of a BOS172767 prototype or matching placebo once daily (QD) or twice daily (BID) for 14 days (Days 1 to 14). |
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| Part 3: Regimen L | Experimental | Participants will be treated with 600 mg of a BOS172767 prototype or matching placebo QD or BID for 14 days (Days 1 to 14). |
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| Part 3: Regimen M | Experimental | Participants will be treated with 800 mg of a BOS172767 prototype or matching placebo QD or BID for 14 days (Days 1 to 14). |
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| BOS172767 liquid capsules | Drug | Oral capsules |
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| BOS172767 micronized capsules | Drug | Oral capsules |
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| BOS172767 immediate release capsules | Drug | Oral capsules |
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| BOS172767 matching placebo capsules | Drug | Oral capsules |
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| BOS172767 matching placebo tablets | Drug | Oral tablets |
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| Rabeprazole | Drug | Oral tablets |
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| Days 1 and 7: pre-dose; 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 16, and 24 hours postdose. Days 4, 6, 9, 11, and 12: pre-dose. Day 14: pre-dose; 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24, 48, 72, 96, and 120 hours post-final dose |
| Part 3 (Regimen M): Plasma concentration of BOS172722 | admission to pre-dose on Day 1; 0 to 6, 6 to 12, and 12 to 24 hours postdose on Days 1, 7, and 14 |
| ID | Term |
|---|---|
| D064750 | Rabeprazole |
| ID | Term |
|---|---|
| D053799 | 2-Pyridinylmethylsulfinylbenzimidazoles |
| D013454 | Sulfoxides |
| D013457 | Sulfur Compounds |
| D009930 | Organic Chemicals |
| D011725 | Pyridines |
| D006573 | Heterocyclic Compounds, 1-Ring |
| D006571 | Heterocyclic Compounds |
| D001562 | Benzimidazoles |
| D006574 | Heterocyclic Compounds, 2-Ring |
| D000072471 | Heterocyclic Compounds, Fused-Ring |
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