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| Name | Class |
|---|---|
| Celerion | INDUSTRY |
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This is a 2-part open-label, randomized, single-dose, 3-sequence, 3-period crossover, relative bioavailability, and food-effect study comparing different formulations of danicopan in healthy adult participants.
For both parts of this study, on Day 1 of each period, participants will receive a single oral dose of danicopan as either the prototype powder-in-capsule (PIC) formulation (1 or 2) under fed conditions, the prototype PIC formulation (1 or 2) under fasting conditions, or the tablet formulation under fed conditions.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Part 1: Sequence 1 | Experimental | Participants will receive danicopan once each period as a single oral dose under fasted or fed conditions as follows: Period 1: Danicopan as the PIC 1 formulation under fed conditions. Period 2: Danicopan as the PIC 1 formulation under fasted conditions. Period 3: Danicopan as a tablet under fed conditions. There will be a washout period of at least 5 days between each danicopan dosing. |
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| Part 1: Sequence 2 | Experimental | Participants will receive danicopan once each period as a single oral dose under fasted or fed conditions as follows: Period 1: Danicopan as the PIC 1 formulation under fasted conditions. Period 2: Danicopan as a tablet under fed conditions. Period 3: Danicopan as the PIC 1 formulation under fed conditions. There will be a washout period of at least 5 days between each danicopan dosing. |
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| Part 1: Sequence 3 | Experimental | Participants will receive danicopan once each period as a single oral dose under fasted or fed conditions as follows: Period 1: Danicopan as a tablet under fed conditions. Period 2: Danicopan as the PIC 1 formulation under fed conditions. Period 3: Danicopan as the PIC 1 formulation under fasted conditions. There will be a washout period of at least 5 days between each danicopan dosing. |
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| Part 2: Sequence 1 | Experimental |
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| Danicopan: Powder-In-Capsule 1 | Drug | Danicopan (200 milligrams) will be administered orally on Day 1. |
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| Measure | Description | Time Frame |
|---|---|---|
| Relative Bioavailability Of Danicopan Prototype PIC 1 Formulation And Tablet Formulation | The relative bioavailability of the PIC 1 formulation versus the tablet formulation will be measured by the ratio of select pharmacokinetic (PK) parameters: maximum observed plasma concentration (Cmax), area under the concentration-time curve from time of administration to the last measurable concentration (AUC0-t), and area under the concentration-time curve from time 0 extrapolated to infinity (AUC0-inf). | Up to 72 hours postdose |
| AUC0-inf Of Danicopan Prototype PIC 1 Formulation Under Both Fed And Fasted Conditions | Up to 72 hours postdose | |
| AUC0-t Of Danicopan Prototype PIC 1 Formulation Under Both Fed And Fasted Conditions | Up to 72 hours postdose | |
| Cmax Of Danicopan Prototype PIC 1 Formulation Under Both Fed And Fasted Conditions | Up to 72 hours postdose | |
| Time to maximum observed plasma concentration (Tmax) Of Danicopan Prototype PIC 1 Formulation Under Both Fed And Fasted Conditions | Up to 72 hours postdose | |
| Relative Bioavailability Of Danicopan Prototype PIC 2 Formulation And Tablet Formulation | The relative bioavailability of the PIC 2 formulation versus the tablet formulation will be measured by the ratio of select PK parameters: Cmax, AUC0-t, and AUC0-inf. | Up to 72 hours postdose |
| AUC0-inf Of Danicopan Prototype PIC 2 Formulation Under Both Fed And Fasted Conditions | Up to 72 hours postdose |
| Measure | Description | Time Frame |
|---|---|---|
| Number Of Participants Receiving Prototype PIC 1 And Tablet With Treatment-emergent Adverse Events Under Fed Conditions | Day 1 (postdose) through follow-up (10 [+/- 2] days dosing on Day 1) | |
| Number Of Participants Receiving Prototype PIC 1 With Treatment-emergent Adverse Events Under Fasted Conditions |
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Inclusion Criteria:
Exclusion Criteria:
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| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Clinical Trial Site | Tempe | Arizona | 85283 | United States |
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| ID | Term |
|---|---|
| C000718467 | danicopan |
| D020742 | rhoA GTP-Binding Protein |
| ID | Term |
|---|---|
| D020741 | rho GTP-Binding Proteins |
| D020559 | Monomeric GTP-Binding Proteins |
| D019204 | GTP-Binding Proteins |
| D020558 | GTP Phosphohydrolases |
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Participants will receive danicopan once each period as a single oral dose under fasted or fed conditions as follows:
Period 1: Danicopan as the PIC 2 formulation under fed conditions. Period 2: Danicopan as the PIC 2 formulation under fasted conditions. Period 3: Danicopan as a tablet under fed conditions.
There will be a washout period of at least 5 days between each danicopan dosing.
|
| Part 2: Sequence 2 | Experimental | Participants will receive danicopan once each period as a single oral dose under fasted or fed conditions as follows: Period 1: Danicopan as the PIC 2 formulation under fasted conditions. Period 2: Danicopan as a tablet under fed conditions. Period 3: Danicopan as the PIC 2 formulation under fed conditions. There will be a washout period of at least 5 days between each danicopan dosing. |
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| Part 2: Sequence 3 | Experimental | Participants will receive danicopan once each period as a single oral dose under fasted or fed conditions as follows: Period 1: Danicopan as a tablet under fed conditions. Period 2: Danicopan as the PIC 2 formulation under fed conditions. Period 3: Danicopan as the PIC 2 formulation under fasted conditions. There will be a washout period of at least 5 days between each danicopan dosing. |
|
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| Danicopan: Powder-In-Capsule 2 | Drug | Danicopan (200 milligrams) will be administered orally on Day 1. |
|
|
| Danicopan: Tablet | Drug | Danicopan (200 milligrams) will be administered orally on Day 1. |
|
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| AUC0-t Of Danicopan Prototype PIC 2 Formulation Under Both Fed And Fasted Conditions | Up to 72 hours postdose |
| Cmax Of Danicopan Prototype PIC 2 Formulation Under Both Fed And Fasted Conditions | Up to 72 hours postdose |
| Tmax Of Danicopan Prototype PIC 2 Formulation Under Both Fed And Fasted Conditions | Up to 72 hours postdose |
| Day 1 (postdose) through follow-up (10 [+/- 2] days dosing on Day 1) |
| Number Of Participants Receiving Prototype PIC 2 And Tablet With Treatment-emergent Adverse Events Under Fed Conditions | Day 1 (postdose) through follow-up (10 [+/- 2] days dosing on Day 1) |
| Number Of Participants Receiving Prototype PIC 2 With Treatment-emergent Adverse Events Under Fasted Conditions | Day 1 (postdose) through follow-up (10 [+/- 2] days dosing on Day 1) |
| D017766 | Acid Anhydride Hydrolases |
| D006867 | Hydrolases |
| D004798 | Enzymes |
| D045762 | Enzymes and Coenzymes |
| D002352 | Carrier Proteins |
| D011506 | Proteins |
| D000602 | Amino Acids, Peptides, and Proteins |
| D047908 | Intracellular Signaling Peptides and Proteins |