Title |
The blood schizonticidal activity of tafenoquine makes an essential contribution to its prophylactic efficacy in nonimmune subjects at the intended dose (200 mg)
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Published in |
Malaria Journal, May 2017
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DOI | 10.1186/s12936-017-1862-4 |
Pubmed ID | |
Authors |
Geoffrey Dow, Bryan Smith |
Abstract |
Tafenoquine (TQ) is an 8-aminoquinoline anti-malarial being developed for malaria prophylaxis. It has been generally assumed that TQ, administered prophylactically, acts primarily on the developing exoerythrocytic stages of malaria parasites (causal prophylaxis), and that polymorphisms in metabolic enzymes thought to impact the activity of other 8-aminoquinolines also inhibit this property of TQ. Furthermore, it has been suggested that a diagnostic test for CYP2D6 metabolizer status might be required. In field studies in which metabolic status was not an exclusion criteria, TQ has been shown to exhibit similar prophylactic efficacy as blood schizonticidal drugs (mefloquine). Also, its blood schizonticidal and anti-relapse efficacy is independent of 2D6 metabolizer status. The most reasonable explanation for the field study results, supported by other clinical and non-clinical data, is that TQ is not completely causal and exhibits substantial blood schizonticidal activity at the intended dose. Pharmacokinetic simulations demonstrate that trough concentrations of TQ exceed the proposed MIC of 80 ng/ml in >95% of individuals. Based on these data a companion diagnostic for CP450 enzyme status is not required. |
X Demographics
Geographical breakdown
Country | Count | As % |
---|---|---|
Australia | 4 | 27% |
Canada | 1 | 7% |
United Kingdom | 1 | 7% |
Unknown | 9 | 60% |
Demographic breakdown
Type | Count | As % |
---|---|---|
Members of the public | 10 | 67% |
Science communicators (journalists, bloggers, editors) | 3 | 20% |
Scientists | 1 | 7% |
Practitioners (doctors, other healthcare professionals) | 1 | 7% |
Mendeley readers
Geographical breakdown
Country | Count | As % |
---|---|---|
Unknown | 27 | 100% |
Demographic breakdown
Readers by professional status | Count | As % |
---|---|---|
Student > Ph. D. Student | 8 | 30% |
Student > Master | 3 | 11% |
Lecturer | 2 | 7% |
Researcher | 2 | 7% |
Student > Bachelor | 2 | 7% |
Other | 3 | 11% |
Unknown | 7 | 26% |
Readers by discipline | Count | As % |
---|---|---|
Medicine and Dentistry | 9 | 33% |
Pharmacology, Toxicology and Pharmaceutical Science | 3 | 11% |
Biochemistry, Genetics and Molecular Biology | 2 | 7% |
Chemistry | 2 | 7% |
Nursing and Health Professions | 1 | 4% |
Other | 1 | 4% |
Unknown | 9 | 33% |