Most Read Articles
3 days ago
Nintedanib does not appear to improve survival in heavily pretreated patients with metastatic colorectal cancer (CRC), according to data from the phase III LUME-Colon 1 trial.
Rachel Soon, 26 Jun 2018

MIMS Pharmacist presents an overview of phosphatidylcholine's physiological role, as well as contemporary research on its pharmacology and effects.

17 Mar 2018
Nonvitamin K antagonist oral anticoagulants (NOAC)-associated intracerebral haemorrhage (ICH) and vitamin K antagonists-ICH appear to have similar ICH volume, haematoma expansion, functional outcome and mortality, results of a recent meta-analysis have shown.
31 May 2017
New drug applications approved by US FDA as of 16 - 31 May 2017 which includes New Molecular Entities (NMEs) and new biologics. It does not include Tentative Approvals. Supplemental approvals may have occurred since the original approval date.

E6201 shows potential in treatment of advanced solid malignancies

12 Jun 2018

A phase I study of E6201 has shown the feasibility and safety of an intermittent regimen of 320 mg/m2 by intravenous (IV) infusion once-weekly (qw) for the first 3 weeks of a 28-day cycle in patients with advanced solid malignancies, including melanoma.

“Additionally, we show preliminary evidence of clinical efficacy, confirming the potential of MEK (mitogen-activated protein kinase/extracellular signal-regulated kinase) inhibition and selective MEK1 inhibition, as a therapeutic strategy in cancer,” the investigators said.

In part A of the study (dose escalation), sequential cohorts received E6201 IV over 30 min qw (days [D]1 + 8 + 15 of a 28-day cycle), starting at 20 mg/m2, increasing to 720 mg/m2 or the maximum tolerated dose (MTD). In part B (expansion), patients with B-type Raf (BRAF)-mutated or wild-type (WT) melanoma received E6201 320 mg/m2 IV over 60 minutes qw (D1 + 8 + 15 of a 28-day cycle) or 160 mg/m2 IV twice-weekly (D1 + 8 + 15 + 18 of a 28-day cycle; BRAF-mutated only).

MTD was 320 mg/m2 qw in part A (n=25) and confirmed in part B (n=30). QT prolongation (n=4) and eye disorders (n=3) were some of the reported adverse events.

There was a dose-related exposure of E6201, with pharmacokinetics characterized by extensive distribution and fast elimination. Partial response was reported in one patient during part A (BRAF-mutated papillary thyroid cancer; 480 mg/m2 qw) and in three during part B (2 BRAF-mutated melanoma; 1 BRAF-WT melanoma; all receiving 320 mg/m2 qw).

“E6201 is being further investigated in a phase I/II trial in patients with advanced haematologic malignancies with the FLT3 mutation,” the investigators said.

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Most Read Articles
3 days ago
Nintedanib does not appear to improve survival in heavily pretreated patients with metastatic colorectal cancer (CRC), according to data from the phase III LUME-Colon 1 trial.
Rachel Soon, 26 Jun 2018

MIMS Pharmacist presents an overview of phosphatidylcholine's physiological role, as well as contemporary research on its pharmacology and effects.

17 Mar 2018
Nonvitamin K antagonist oral anticoagulants (NOAC)-associated intracerebral haemorrhage (ICH) and vitamin K antagonists-ICH appear to have similar ICH volume, haematoma expansion, functional outcome and mortality, results of a recent meta-analysis have shown.
31 May 2017
New drug applications approved by US FDA as of 16 - 31 May 2017 which includes New Molecular Entities (NMEs) and new biologics. It does not include Tentative Approvals. Supplemental approvals may have occurred since the original approval date.