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Also known as Selumetinib, Selumetinib capsule formulation, Selumetinib formulation
selumetinib single dose · 2 trials · 2 indications
The bioequivalence of the free base variant of selumetinib (Treatment B) as compared to the blue reference capsule (Treatment A) was evaluated by comparing the maximum observed plasma concentration (Cmax) of selumetinib in healthy volunteers.
The bioequivalence of the free base variant of selumetinib (Treatment B) as compared to the blue reference capsule (Treatment A) was evaluated by comparing the area under the plasma concentration-time curve from time zero extrapolated to infinity (AUC) of selumetinib in healthy volunteers.
The bioequivalence of the free base variant of selumetinib (Treatment B) as compared to the blue reference capsule (Treatment A) was evaluated by comparing the AUC from time zero to the time of the last quantifiable concentration (AUC\[0-t\]) of selumetinib in healthy volunteers.
To calculate absolute bioavailability we used the formula: Area Under the Curve (oral dose)/Area Under the Curve (intravenous dose)\*100
| Arm | Type | Description |
|---|---|---|
| Treatment A | EXPERIMENTAL | AZD6244 blue reference capsules (3 x 25 mg) administered orally |
| Treatment B | EXPERIMENTAL | AZD6244 blue capsules (3 x 25 mg) Variant 1 (free base variant) administered orally |
| Treatment C | EXPERIMENTAL | AZD6244 blue capsules (3 x 25 mg) Variant 2 (vitamin E polyethylene glycol succinate \[TPGS\] variant) administered orally |
| selumetinib 75mg single dose | EXPERIMENTAL | 3 capsules of 25 mg administered orally |
| Name | Type | Description |
|---|---|---|
| selumetinib 75mg single dose | DRUG | 3 blue capsules of 25 mg given as a single dose |
| [14C] selumetinib IV solution | OTHER | single, radiolabeled, IV (infused), microdose (80 μg) of \[14C\] selumetinib, infused using a syringe pump as a 15-minute infusion, administered 1h 15 min after receiving the oral dose |
Inclusion Criteria:1.Provision of written informed consent 2.Healthy male volunteers aged 18 to 45 years 3.Calculated creatinine clearance (CrCL) \>50 mL/minute using the Cockcroft-Gault formula 4.Healthy volunteers with sexual partners who could become pregnant should agree to use 2 highly effectiv...
Selumetinib is an investigational small molecule being studied for several cancers, including locally advanced or metastatic non-small cell lung cancer (NSCLC) stage IIIB-IV, solid tumors, neurofibromatosis type 1, and lung cancer. It is also being evaluated in metastatic uveal melanoma. Selumetinib is not FDA approved and remains in clinical development.
Selumetinib is a kinase inhibitor, belonging to the -tinib class of drugs. It works by inhibiting specific kinase enzymes involved in cell signaling pathways that promote tumor growth. The drug is being studied in combination with docetaxel for the treatment of KRAS-positive NSCLC and other advanced cancers.
Selumetinib is being developed by AstraZeneca PLC, a biopharmaceutical company listed on the stock exchange under the ticker symbol AZN. AstraZeneca is conducting clinical trials to evaluate the safety and efficacy of Selumetinib in various cancer indications.
Selumetinib is in Phase 1 clinical development. While some trials have reached Phase 2 and Phase 3, the drug's overall development stage is Phase 1. It is an investigational drug and has not received FDA approval for any indication.
Selumetinib has been studied in multiple clinical trials, including NCT01750281, a Phase 2 trial combining Selumetinib with docetaxel in second-line NSCLC patients, and NCT01933932, a Phase 3 trial in KRAS-positive NSCLC. Other trials include NCT01960374, a Phase 1 pharmacokinetic study in healthy volunteers, and NCT01974752, a Phase 3 trial in metastatic uveal melanoma.
Yes, Selumetinib is also known as Selumetinib capsule formulation and Selumetinib formulation. These names refer to the same drug substance, which is being developed by AstraZeneca for the treatment of various cancers, including NSCLC and neurofibromatosis type 1.