Approval Probability
TA Base Rate
Adjusted LOA
ML Risk
ALXN2050 · 8 trials · 2 indications
see Time Frame - defined
see Time Frame - defined
see Time Frame - defined
see Time Frame - defined
see Time Frame - defined
see Time Frame - defined
see Time Frame - defined
Mass balance will be assessed by evaluating total radioactivity recovery and the percent of the radioactive dose excreted in the urine and feces. Mass balance will be calculated as a sum of the percent of the total radioactivity recovered in urine and feces plus any radioactivity dose lost due to emesis (if any occurred) relative to the administered radioactivity dose.
ALXN2050 metabolic profiling in plasma, urine, and feces will be performed in samples containing sufficient amounts of radioactivity. The percent of dose represented by each of the metabolites will be calculated using the radioactivity concentration equivalent data combined with the metabolic profiling data. The percentage of each identified metabolite to total radioactivity in plasma will be estimated based on plasma metabolic profiling data.
Twelve-lead electrocardiograms (ECGs) will be extracted from continuous (Holter) recordings.
| Arm | Type | Description |
|---|---|---|
| Part 1 - Cyclosporine | EXPERIMENTAL | Participants will receive ALXN2050 and cyclosporine in a fixed sequence over 3 periods. Period 1: Participants will receive multiple doses of ALXN2050. Period 2: Participants will receive multiple doses of cyclosporine. Period 3: Participants will receive multiple doses of ALXN2050 co-administered with multiple doses of cyclosporine. There will be a washout period between the last dose of ALXN2050 in Period 1 and the first dose of cyclosporine in Period 2 and between the last dose of cyclosporine in Period 2 and the first dosing in Period 3. |
| Part 2 - Tacrolimus | EXPERIMENTAL | Participants will receive tacrolimus and ALXN2050 in a fixed sequence over 2 periods. Period 1: Participants will receive a single dose of tacrolimus. Period 2: Participants will receive multiple doses of ALXN2050 alone and co-administered with a single dose of tacrolimus. There will be a washout period between the dose of tacrolimus in Period 1 and the first dose of ALXN2050 in Period 2. |
| Part 3 - MMF | EXPERIMENTAL | Participants will receive MMF and ALXN2050 in a fixed sequence over 2 periods. Period 1: Participants will receive a single dose of MMF. Period 2: Participants will receive multiple doses of ALXN2050 alone and co-administered with a single dose of MMF. There will be a washout period between the dose of MMF in Period 1 and the first dose of ALXN2050 in Period 2. |
| Cohort 1: ALXN2050 (Dose 1) | EXPERIMENTAL | Participants will receive ALXN2050 (Dose 1) as follows under fasting conditions: 120-milligrams (mg) single dose, 3-day washout, then 120-mg twice daily (BID) dosing. |
| Cohort 1: Placebo (Dose 1) | EXPERIMENTAL | Participants will receive placebo (Dose 1) as follows under fasting conditions: 120-mg placebo single dose, 3-day washout, then 120-mg placebo BID dosing. |
| Cohort 2: ALXN2050 (Dose 2) | EXPERIMENTAL | Participants will receive ALXN2050 (Dose 2) as follows under fasting conditions: 180-mg single dose, 3-day washout, then 180-mg BID dosing. |
| Cohort 2: Placebo (Dose 2) | EXPERIMENTAL | Participants will receive placebo (Dose 2) as follows under fasting conditions: 180-mg placebo single dose, 3-day washout, then 180-mg placebo BID dosing. |
| Cohort 1: Severe Impaired Renal Function | EXPERIMENTAL | Participants will receive ALXN2050. |
| Cohort 2: Moderate Impaired Renal Function | EXPERIMENTAL | Participants will receive ALXN2050. |
| Cohort 3: Mild Impaired Renal Function | EXPERIMENTAL | Participants will receive ALXN2050. |
| Cohort 4: Healthy Control | EXPERIMENTAL | Participants will receive ALXN2050. |
| Part 1: ALXN2050 plus Fluconazole | EXPERIMENTAL | Period 1: Participants will receive a single dose of ALXN2050 alone and in the presence of multiple doses of fluconazole. Period 2: Participants will receive multiple doses of ALXN2050 alone and in the presence of multiple doses of fluconazole. Scheduled pharmacokinetics (PK) blood samples for both ALXN2050 and fluconazole will be collected, with a washout period of at least 14 days between the last dose of fluconazole in Period 1 and the first dose of ALXN2050 in Period 2. |
| Part 2: ALXN2050 plus Rifampin | EXPERIMENTAL | Participants will receive a single dose of ALXN2050 alone and in the presence of both single and multiple doses of rifampin. Scheduled PK blood samples for both ALXN2050 and rifampin will be collected. |
| [14C]-ALXN2050 | EXPERIMENTAL | Participants will receive \[14C\]-ALXN2050. |
| Treatment Arm (ABC) | EXPERIMENTAL | Treatment Sequence ABC - Participants will receive all 3 doses of ALXN2050 in a multiple-ascending fashion over 3 periods: Treatment A (Period 1): ALXN2050 Dose 120 milligrams (mg) and moxifloxacin-matching placebo. Treatment B (Period 2): ALXN2050 Dose 240 mg and moxifloxacin-matching placebo. Treatment C (Period 3): ALXN2050 Dose 360 mg and moxifloxacin-matching placebo. |
| Control Arm (DEF) | PLACEBO_COMPARATOR | Treatment Sequence DEF - Participants will receive ALXN2050-matching placebo over 3 periods: Treatment D (Period 1): 120 mg ALXN2050-matching placebo and moxifloxacin-matching placebo. Treatment E (Period 2): 240 mg ALXN2050-matching placebo and moxifloxacin. Treatment F (Period 3): 360 mg ALXN2050-matching placebo and moxifloxacin-matching placebo. |
| Control Arm (GHI) | PLACEBO_COMPARATOR | Treatment Sequence GHI - Participants will receive ALXN2050-matching placebo over 3 periods: Treatment G (Period 1): 120 mg ALXN2050-matching placebo and moxifloxacin. Treatment H (Period 2): 240 mg ALXN2050-matching placebo and moxifloxacin-matching placebo. Treatment I (Period 3): 360 mg ALXN2050-matching placebo and moxifloxacin. |
| Cohort 1: 40 mg ALXN2050/Placebo | EXPERIMENTAL | Participants randomized to receive ALXN2050 or placebo twice daily (BID) on Day 1 through Day 14 in a fasted state. |
| Cohort 2: 80 mg ALXN2050/Placebo | EXPERIMENTAL | Participants randomized to receive ALXN2050 or placebo BID on Day 1 through Day 14 in a fasted state. |
| Cohort 3: 120 mg ALXN2050/Placebo | EXPERIMENTAL | Participants randomized to receive ALXN2050 or placebo BID on Day 1 through Day 14 in a fasted state. |
| Cohort 4: 200 mg ALXN2050/Placebo | EXPERIMENTAL | Participants randomized to receive ALXN2050 or placebo BID on Day 1 through Day 14 in a fasted state. |
| Cohort 5: 120 mg ALXN2050/Placebo | EXPERIMENTAL | Participants randomized to receive a single dose of ALXN2050 or placebo on Day 1 in a fed state. |
| Cohort 6: 240 mg ALXN2050/Placebo | EXPERIMENTAL | Participants randomized to receive a single dose of ALXN2050 or placebo on Day 1 in a fasted state. |
| Name | Type | Description |
|---|---|---|
| ALXN2050 | DRUG | Oral tablet. |
| Cyclosporine | DRUG | Oral capsule. |
| Tacrolimus | DRUG | Oral capsule. |
| MMF | DRUG | Oral tablet. |
| Placebo | DRUG | Oral tablet. |
| Fluconazole | DRUG | Oral tablet. |
| Rifampin | DRUG | Oral capsule. |
| [14C]-ALXN2050 | DRUG | A single dose of 200 milligrams (\~85 microcuries) \[14C\]-ALXN2050 will be administered orally. |
| ALXN2050-matching Placebo | DRUG | ALXN2050-matching placebo will be administered orally twice daily as placebo powder-in-capsule. |
| Moxifloxacin | DRUG | Moxifloxacin will be administered as a single oral dose. |
| Moxifloxacin-matching Placebo | DRUG | Moxifloxacin-matching placebo will be administered as a single oral dose. |
Inclusion Criteria: * Medically healthy with no clinically significant or relevant abnormalities as determined by medical history, physical or neurological examination, vital signs, 12-lead electrocardiogram, screening clinical laboratory profiles (hematology, biochemistry, coagulation, and urinaly...
ALXN2050 is an investigational small molecule being studied in healthy volunteers and in people with renal impairment. It is in Phase 1 clinical development. The drug is being evaluated for its safety, tolerability, and pharmacological effects, including cardiac effects and potential drug-drug interactions.
ALXN2050 is being developed by AstraZeneca PLC, which trades under the ticker AZN. The company is conducting Phase 1 clinical trials to evaluate the drug's safety and tolerability in healthy participants and in individuals with renal impairment.
ALXN2050 is in Phase 1 clinical development. It is an investigational drug, meaning it has not been approved by regulatory authorities. All seven clinical trials for ALXN2050 have been completed, with no active trials currently ongoing.
ALXN2050 has been studied in seven completed Phase 1 clinical trials. These include NCT04660890, a cardiac effects study in healthy adults; NCT04952545, a study in healthy Japanese adults; NCT05047458, a single-dose study in healthy adults; and NCT05202145, a drug-drug interaction study.
ALXN2050 is a small molecule, but its specific molecular target has not been disclosed in the available clinical trial information. The ongoing and completed Phase 1 studies focus on evaluating its safety, tolerability, and pharmacokinetics in healthy participants and those with renal impairment.