Most Read Articles
Prof. Cheuk-Chun Szeto, Dr. Winston W. S. Fung, 25 Jan 2018
A 65-year-old lady with a background of type 2 diabetes, hyperlipidaemia and chronic immune thrombocytopenia presented to us with a 2-week history of generalized malaise and myalgia. Shortly after the onset of myalgia, she was noted to have reduced urine output and the urine was described as dark in colour. Her regular medications included prednisolone, danazol, simvastatin, metformin, and human insulin. Upon further questioning, the patient admitted that her compliance to simvastatin and danazol used to be poor. However, she recently started to take both medications regularly after repeated education.
Pearl Toh, 30 Jan 2018
Use of statins may not be neuroprotective, in contrast to findings from previous observational studies. On the contrary, fungus-derived or lipophilic statins appeared to be associated with a slightly increased risk of Alzheimer's disease (AD) compared with synthetic and hydrophilic statins, suggests a new study based on real-world clinical practice data.
26 Dec 2017
Supplementation with omega-3 fatty acids in combination with rosuvastatin may yield significant reductions in triglycerides and nonhigh-density lipoprotein (HDL) cholesterol as compared with rosuvastatin monotherapy, according to data from the ROMANTIC (rosuvastatin-omacor in residual hypertriglyceridemia) trial.
Rachel Soon, 21 Feb 2018

MIMS Pharmacist sits down with pharmacist researcher Dr Mai Chun Wai to find out more about his work in drug discovery, including his investigations of Antarctic soil microorganisms.

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
Prof. Cheuk-Chun Szeto, Dr. Winston W. S. Fung, 25 Jan 2018
A 65-year-old lady with a background of type 2 diabetes, hyperlipidaemia and chronic immune thrombocytopenia presented to us with a 2-week history of generalized malaise and myalgia. Shortly after the onset of myalgia, she was noted to have reduced urine output and the urine was described as dark in colour. Her regular medications included prednisolone, danazol, simvastatin, metformin, and human insulin. Upon further questioning, the patient admitted that her compliance to simvastatin and danazol used to be poor. However, she recently started to take both medications regularly after repeated education.
Pearl Toh, 30 Jan 2018
Use of statins may not be neuroprotective, in contrast to findings from previous observational studies. On the contrary, fungus-derived or lipophilic statins appeared to be associated with a slightly increased risk of Alzheimer's disease (AD) compared with synthetic and hydrophilic statins, suggests a new study based on real-world clinical practice data.
26 Dec 2017
Supplementation with omega-3 fatty acids in combination with rosuvastatin may yield significant reductions in triglycerides and nonhigh-density lipoprotein (HDL) cholesterol as compared with rosuvastatin monotherapy, according to data from the ROMANTIC (rosuvastatin-omacor in residual hypertriglyceridemia) trial.
Rachel Soon, 21 Feb 2018

MIMS Pharmacist sits down with pharmacist researcher Dr Mai Chun Wai to find out more about his work in drug discovery, including his investigations of Antarctic soil microorganisms.