Approval Probability
TA Base Rate
Adjusted LOA
ML Risk
AZD6244 · 11 trials · 19 indications
Following progression survival data was collected until documentation of death, withdrawal of consent, loss to follow-up or the final data cut-off, whichever occurred first.
The TTD (days) was calculated as the interval from date of randomisation to date of patient death (from any cause). Patients who had not died at the time of the final analysis were censored at the last date the patient was known to be alive. Median TTD in days is presented here.
Pharmacokinetic parameter (Cmax: maximum plasma concentration) of Selumetinib following single oral dose of Selumetinib
Pharmacokinetic parameter (tmax: time to reach the maximum plasma concentration) of Selumetinib following single oral dose of Selumetinib
Pharmacokinetic parameter (AUC(0-12): area under the plasma concentration-time curve from zero to 12 hours post-dosey) of Selumetinib following single oral dose of Selumetinib
Pharmacokinetic parameter (Cmax: maximum plasma concentration) of N-desmethyl Selumetinib following single oral dose of Selumetinib
Pharmacokinetic parameter (tmax: time to reach the maximum plasma concentration) of N-desmethyl Selumetinib following single oral dose of Selumetinib
Pharmacokinetic parameter (AUC(0-12): area under the plasma concentration-time curve from zero to 12 hours post-dose) of N-desmethyl Selumetinib following single oral dose of Selumetinib
Pharmacokinetic parameter (Cmax: maximum plasma concentration) of Selumetinib during oral twice daily dose of Selumetinib
Pharmacokinetic parameter (tmax: time to reach the maximum plasma concentration) of Selumetinib during oral twice daily dose of Selumetinib
Pharmacokinetic parameter (AUC(0-12): area under the plasma concentration-time curve from zero to 12 hours post-dose) of Selumetinib during oral twice daily dose of Selumetinib
Pharmacokinetic parameter (Cmax: maximum plasma concentration) of N-desmethyl Selumetinib during oral twice daily dose of Selumetinib
Pharmacokinetic parameter (tmax: time to reach the maximum plasma concentration) of N-desmethyl Selumetinib during oral twice daily dose of Selumetinib
Pharmacokinetic parameter (AUC(0-12): area under the plasma concentration-time curve from zero to 12 hours post-dose) of N-desmethyl Selumetinib during oral twice daily dose of Selumetinib
Incidence and intensity of adverse events as graded by CTCAE (version 3.0), physical examinations, vital signs (including weight, blood pressure and pulse rate), ECG parameters, MUGA scan and echocardiography, clinical chemistry (including liver function tests), Brain Natriuretic Peptide (BNP), Troponin I, hematology, urinalysis, and ophthalmologic examinations.
An adverse event (AE) is any untoward medical occurrence in a participant who received study drug without regard to possibility of causal relationship. A serious adverse event (SAE) is an AE resulting in any of the following outcomes or deemed significant for any other reason: death; initial or prolonged inpatient hospitalization; life threatening experience (immediate risk of dying); persistent or significant disability/incapacity; congenital anomaly. The TEAEs are defined as events present at baseline that worsened in intensity after administration of study drug or events absent at baseline that emerged after administration of study drug.
Number of participants with abnormal clinical laboratory parameters reported as TEAEs are reported. Abnormal clinical laboratory parameters defined as any abnormal finding during analysis of hematology, clinical chemistry, and urinalysis.
Number of participants with abnormal vital signs reported as TEAEs are reported. Abnormal vital signs are defined as any abnormal finding in the vital sign parameters (blood pressure, oxygen saturation, weight, and pulse rate).
Number of participants with abnormal ECHO parameters reported as TEAEs are reported.
Number of participants with abnormal ECG parameters reported as TEAEs are reported.
| Arm | Type | Description |
|---|---|---|
| 1 | EXPERIMENTAL | Selumetinib (AZD6244) in combination with irinotecan |
| 2 | PLACEBO_COMPARATOR | Placebo in combination with dacarbazine |
| AZD6244 + Docetaxel | ACTIVE_COMPARATOR | AZD6244 75 mg bd + Docetaxel 75 mg/m\^2 |
| Placebo + Docetaxel | PLACEBO_COMPARATOR | Placebo + Docetaxel 75 mg/m\^2 |
| Selumetinib (AZD6244) 25 mg | EXPERIMENTAL | monotherapy |
| Selumetinib (AZD6244) 50 mg | EXPERIMENTAL | monotherapy |
| Selumetinib (AZD6244) 75 mg | EXPERIMENTAL | monotherapy |
| Selumetinib (AZD6244) 75 mg + Doce | EXPERIMENTAL | Combination |
| Selumetinib (AZD6244) 25 mg + Doce | EXPERIMENTAL | combination |
| 3 | EXPERIMENTAL | AZD6244 + Erlotinib |
| 4 | EXPERIMENTAL | AZD6244 + Temsirolimus |
| Part A: Dose Escalation AZD6244 25 mg | EXPERIMENTAL | Participants will receive a single oral dose of AZD6244 25 mg capsule on Day 1 followed by continuous twice daily (bd) dosing from Day 2 onwards, until disease progression or another protocol-defined discontinuation criterion will be met, whichever will occur first. |
| Part A: Dose Escalation AZD6244 50 mg | EXPERIMENTAL | Participants will receive a single oral dose of AZD6244 50 mg capsule on Day 1 followed by continuous dosing from Day 2 onwards, until disease progression or another protocol-defined discontinuation criterion will be met, whichever will occur first. |
| Part A: Dose Escalation AZD6244 75 mg | EXPERIMENTAL | Participants will receive a single oral dose of AZD6244 75 mg capsule on Day 1 followed by continuous dosing from Day 2 onwards, until disease progression or another protocol-defined discontinuation criterion will be met, whichever will occur first. |
| Part A: Dose Escalation AZD6244 100 mg | EXPERIMENTAL | Participants will receive a single oral dose of AZD6244 100 mg capsule on Day 1 followed by continuous dosing from Day 2 onwards, until disease progression or another protocol-defined discontinuation criterion will be met, whichever will occur first. |
| Part B: Relative Bioavailability (Sequence 1) and Safety Assessment Phase | EXPERIMENTAL | Participants in relative bioavailability phase will receive a single oral dose of AZD6244 100 mg free-base suspension (mix and drink) on Day 1. Following a washout period of 7 days, participants will receive a single oral dose of AZD6244 75 mg capsule on Day 8 (Sequence 1). In the safety assessment phase, participants who will participate in the relative bioavailability phase will receive oral AZD6244 75 mg capsule bd dosing from Day 9 onwards until disease progression or another protocol-defined discontinuation criterion will be met, whichever will occur first. |
| Part B: Relative Bioavailability (Sequence 2) and Safety Assessment Phase | EXPERIMENTAL | Participants in relative bioavailability phase will receive a single oral dose of AZD6244 75 mg capsule on Day 1. Following a washout period of 7 days, participants will receive a single oral dose of AZD6244 100 mg free-base suspension (mix and drink) on Day 8 (Sequence 2). In the safety assessment phase, participants who will participate in the relative bioavailability phase will receive oral AZD6244 75 mg capsule bd dosing from Day 9 onwards until disease progression or another protocol-defined discontinuation criterion will be met, whichever will occur first. |
| Name | Type | Description |
|---|---|---|
| AZD6244 | DRUG | 50 or 75mg, capsules, PO, BID, 28 days |
| Irinotecan | DRUG | 180mg/m2, IV, Day 1\& 15 of each cycle |
| Dacarbazine | DRUG | 1000 mg/m2 iv infusion over at least 60 min. on day 1 of each 21 cycle |
| Placebo | DRUG | Placebo |
| docetaxel | DRUG | 75mg/m2 iv on day 1 of every 21 day cycle |
| Capecitabine | DRUG | oral tablet |
| Pemetrexed | DRUG | oral |
| Temozolomide | DRUG | oral |
| Erlotinib | DRUG | daily oral dose |
| Temsirolimus | DRUG | intravenous infusion |
Inclusion Criteria: \- Histological or cytological confirmation of advanced or metastatic colorectal cancer with available tissue and tumor sample confirmed as K-ras or B-raf mutation positive. Current failure of 1st line anti-cancer therapy with an oxaliplatin and bevacizumab based regimen or pati...
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AZD6244 is an investigational small molecule being studied in oncology for advanced solid malignancies and specific cancers including non-small cell lung cancer, pancreatic cancer, melanoma, and metastatic colorectal cancer. It is currently in Phase 1 clinical development and has not been approved by regulatory authorities.
AZD6244 is a small molecule that targets the MEK pathway, which is involved in cell growth and proliferation. By inhibiting this pathway, the drug aims to slow or stop the growth of cancer cells. This mechanism is being evaluated in clinical trials for various solid tumors.
AZD6244 is being developed by AstraZeneca PLC, a biopharmaceutical company listed on the stock exchange under the ticker symbol AZN. The company is conducting clinical trials to evaluate the safety and efficacy of this investigational drug in patients with advanced cancers.
AZD6244 is currently in Phase 1 clinical development. It is an investigational drug, meaning it has not yet received approval from regulatory agencies such as the FDA. The drug is being studied in early-stage trials to assess its safety, tolerability, and pharmacokinetics in patients with advanced solid tumors.
AZD6244 has been studied in several clinical trials, including NCT00463814, a Phase 1 study in advanced solid malignancies, and NCT00600496, a Phase 1 trial in various cancers. A Phase 2 trial, NCT00890825, evaluated AZD6244 with docetaxel in KRAS mutation positive NSCLC patients. Another Phase 1 trial, NCT01605916, was conducted in Japanese patients.
Yes, AZD6244 is also known as ARRY-142886. Clinical trial records refer to the drug by both names, such as in the study titled 'AZD6244 (ARRY-142886) Solid Oral Dosage Formulation in Participants With Advanced Solid Malignancies.' This alternative name is used interchangeably in research documentation.