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| Name | Class |
|---|---|
| Purdue Pharma LP | INDUSTRY |
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This study will be conducted to evaluate the effect of lemborexant 10 milligrams (mg) (at steady state) on the pharmacokinetics (PK) of a single-dose combined oral contraceptive, Loestrin 1.5/30 (containing 0.030 mg of ethinyl estradiol and 1.5 mg of norethindrone), and to evaluate the effect of fluconazole 200 mg (at steady state) and a single dose of famotidine 40 mg (an H2 blocker) on the PK of a single oral dose of lemborexant 10 mg.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Part 1: Lemborexant plus Loestrin | Experimental | Healthy female participants will receive a single oral dose of Loestrin 1.5/30 (containing ethinyl estradiol [EE] 0.030 milligrams [mg] and norethindrone [NE] 1.5 mg) in the evening of Day 1 after a fast of at least 3 hours. After a washout period of at least 4 days, participants will receive 10 mg lemborexant orally for 10 days. Lemborexant will continue to be administered in the evening on Days 15 through 18, followed by a single oral dose of Loestrin on Day 15 when administered with lemborexant after fasting in the evening for at least 3 hours. |
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| Part 2: Lemborexant plus Famotidine | Experimental | Healthy participants will receive a single oral dose of 10 mg lemborexant in the morning of Day 1 after an overnight fast of at least 10 hours. On Day 15, participants will receive a single oral dose of 40 mg famotidine, followed at least 2 hours later by a single dose of 10 mg lemborexant. After a washout period of up to 14 days participants will receive 10 mg lemborexant orally for 10 days. |
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| Part 3: Lemborexant plus Fluconazole | Experimental | Healthy participants will receive a single oral dose of 10 mg lemborexant in the morning of Day 1 after an overnight fast of at least 10 hours. After a washout interval of approximately 10 days, on Day 11, participants will be administered 400 mg fluconazole followed by 200 mg fluconazole once daily from Days 12 to 26. During this time a single dose of 10 mg lemborexant will be administered following an overnight fast of at least 10 hours along with fluconazole on Day 15 only. |
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| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| lemborexant | Drug | oral tablet |
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| Measure | Description | Time Frame |
|---|---|---|
| Part 1 (Lemborexant plus Loestrin): Mean maximum observed concentration (Cmax) of lemborexant and metabolites | Blood samples for lemborexant and metabolite assessment will be obtained at predose and 0.5 (30 minutes), 1, 1.5, 2, 3, 4, 5, 6, 8, 12, and 24 hours postdose on Days 14 and 15. | |
| Part 1 (Lemborexant plus Loestrin): Mean predose drug concentration (Cmin) of lemborexant and metabolites | Blood samples for lemborexant and metabolite assessment will be obtained at predose and 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, and 24 hours postdose on Days 14 and 15. | |
| Part 1 (Lemborexant plus Loestrin): Mean time to reach maximum (peak) drug concentration following drug administration (Tmax) of lemborexant and metabolites | Blood samples for lemborexant and metabolite assessment will be obtained at predose and 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, and 24 hours postdose on Days 14 and 15. | |
| Part 1 (Lemborexant plus Loestrin): Mean area under the concentration-time curve from zero time to 24 hours postdose (AUC[0-24h]) of lemborexant and metabolites | Blood samples for lemborexant and metabolite assessment will be obtained at predose and 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, and 24 hours postdose on Days 14 and 15. | |
| Part 2 (Lemborexant plus Famotidine): Mean Cmax of lemborexant and metabolites | Blood samples for lemborexant and metabolite assessment will be obtained at predose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48, 72, 120, 168, and 216 hours after dosing on Days 1 and 15. | |
| Part 2 (Lemborexant plus Famotidine): Mean Tmax of lemborexant and metabolites | Blood samples for lemborexant and metabolite assessment will be obtained at predose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48, 72, 120, 168, and 216 hours after dosing on Days 1 and 15. |
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Inclusion Criteria:
Inclusion Criteria for All Participants (Part 1 - Oral Contraceptive; Part 2 - Famotidine; Part 3 - Fluconazole)
Participants who meet all of the following inclusion criteria will be eligible for participation in the study:
Additional Inclusion Criteria for Part 1 - Oral Contraceptive
Additional Inclusion Criteria (Part 2 - Famotidine; Part 3 - Fluconazole)
-Healthy male or female, age ≥18 years and ≤55 years old at the time of informed consent
Exclusion Criteria:
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| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Worldwide Clinical Trials | San Antonio | Texas | 78217 | United States |
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|
| Loestrin | Drug | oral tablet |
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| famotidine | Drug | oral tablet |
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| fluconazole | Drug | oral tablet |
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| Part 2 (Lemborexant plus Famotidine): Mean AUC(0-24h) of lemborexant and metabolites | Blood samples for lemborexant and metabolite assessment will be obtained at predose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48, 72, 120, 168, and 216 hours after dosing on Days 1 and 15. |
| Part 2 (Lemborexant plus Famotidine): Mean AUC from zero time to 72 hours postdose (AUC[0-72h]) of lemborexant and metabolites | Blood samples for lemborexant and metabolite assessment will be obtained at predose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48, 72, 120, 168, and 216 hours after dosing on Days 1 and 15. |
| Part 2 (Lemborexant plus Famotidine): Mean AUC from zero time to last measurable time (AUC[0-t]) of lemborexant and metabolites | Blood samples for lemborexant and metabolite assessment will be obtained at predose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48, 72, 120, 168, and 216 hours after dosing on Days 1 and 15. |
| Part 2 (Lemborexant plus Famotidine): Mean AUC from zero time extrapolated to infinite time (AUC[0-inf]) of lemborexant and metabolites | Blood samples for lemborexant and metabolite assessment will be obtained at predose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48, 72, 120, 168, and 216 hours after dosing on Days 1 and 15. |
| Part 2 (Lemborexant plus Famotidine): Mean terminal elimination half-life (t1/2) of lemborexant and metabolites following the last dose | Blood samples for lemborexant and metabolite assessment will be obtained at predose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48, 72, 120, 168, and 216 hours after dosing on Days 1 and 15. |
| Part 3 (Lemborexant plus Fluconazole): Mean Cmax of lemborexant and metabolites | Day 1 at predose and at approximately 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 12 hours postdose. At approximately 24, 48, and 72 (Days 2 to 4); 120 (Day 6); 168 (Day 8); 216 (Day 10) hours after the first dose. Day 15 at predose and at approximately 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 12 hours after the second dose. At approximately 24, 48, and 72 (Days 16 to 18); 120 (Day 20); 168 (Day 22); 216 (Day 24); 288 (Day 27) hours after the second dose. | Blood samples for lemborexant and metabolite assessment will be obtained on Days 1 to 27. |
| Part 3 (Lemborexant plus Fluconazole): Mean Tmax of lemborexant and metabolites | Day 1 at predose and at approximately 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 12 hours postdose. At approximately 24, 48, and 72 (Days 2 to 4); 120 (Day 6); 168 (Day 8); 216 (Day 10) hours after the first dose. Day 15 at predose and at approximately 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 12 hours after the second dose. At approximately 24, 48, and 72 (Days 16 to 18); 120 (Day 20); 168 (Day 22); 216 (Day 24); 288 (Day 27) hours after the second dose. | Blood samples for lemborexant and metabolite assessment will be obtained on Days 1 to 27. |
| Part 3 (Lemborexant plus Fluconazole): Mean AUC(0-24h) of lemborexant and metabolites | Day 1 at predose and at approximately 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 12 hours postdose. At approximately 24 (Day 2) hours after the first dose. Day 15 at predose and at 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 12 hours after the second dose. At approximately 24 (Day 16) hours after the second dose. | Blood samples for lemborexant and metabolite assessment will be obtained on Days 1 to 16. |
| Part 3 (Lemborexant plus Fluconazole): Mean AUC(0-72h) of lemborexant and metabolites | Day 1 at predose and at approximately 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 12 hours postdose. At approximately 24, 48, and 72 (Days 2 to 4) hours after the first dose. Day 15 at predose and at 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 12 hours after the second dose. At approximately 24, 48, 72 hours (Days 16 to 18 after the second dose). | Blood samples for lemborexant and metabolite assessment will be obtained on Days 1 to 18. |
| Part 3 (Lemborexant plus Fluconazole): Mean AUC(0-t) of lemborexant and metabolites | Day 1 at predose and at approximately 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 12 hours postdose. At approximately 24, 48, and 72 (Days 2 to 4); 120 (Day 6); 168 (Day 8); 216 (Day 10) hours after the first dose. Day 15 at predose and at approximately 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 12 hours after the second dose. At approximately 24, 48, and 72 (Days 16 to 18); 120 (Day 20); 168 (Day 22); 216 (Day 24); 288 (Day 27) hours after the second dose. | Blood samples for lemborexant and metabolite assessment will be obtained on Days 1 to 27. |
| Part 3 (Lemborexant plus Fluconazole): Mean AUC(0-inf) of lemborexant and metabolites | Day 1 at predose and at approximately 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 12 hours postdose. At approximately 24, 48, and 72 (Days 2 to 4); 120 (Day 6); 168 (Day 8); 216 (Day 10) hours after the first dose. Day 15 at predose and at approximately 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 12 hours after the second dose. At approximately 24, 48, and 72 (Days 16 to 18); 120 (Day 20); 168 (Day 22); 216 (Day 24); 288 (Day 27) hours after the second dose. | Blood samples for lemborexant and metabolite assessment will be obtained on Days 1 to 27. |
| Part 3 (Lemborexant plus Fluconazole): Mean t1/2 of lemborexant and metabolites following last dose | Day 1 at predose and at approximately 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 12 hours postdose. At approximately 24, 48, and 72 (Days 2 to 4); 120 (Day 6); 168 (Day 8); 216 (Day 10) hours after the first dose. Day 15 at predose and at approximately 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 12 hours after the second dose. At approximately 24, 48, and 72 (Days 16 to 18); 120 (Day 20); 168 (Day 22); 216 (Day 24); 288 (Day 27) hours after the second dose. | Blood samples for lemborexant and metabolite assessment will be obtained on Days 1 to 27. |
| ID | Term |
|---|---|
| C000634104 | lemborexant |
| C020416 | norethindrone acetate, ethinyl estradiol, ferrous fumarate drug combination |
| D015738 | Famotidine |
| D015725 | Fluconazole |
| ID | Term |
|---|---|
| D013844 | Thiazoles |
| D013457 | Sulfur Compounds |
| D009930 | Organic Chemicals |
| D001393 | Azoles |
| D006573 | Heterocyclic Compounds, 1-Ring |
| D006571 | Heterocyclic Compounds |
| D014230 | Triazoles |
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