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Okada K, Sato A, Hiramoto A, et al. Pharmacokinetic analysis of new synthetic antimalarial N-251. Trop Med Health. 2019;47:40doi: 10.1186/s41182-019-0167-4.
Okada, K., Sato, A., Hiramoto, A., Isogawa, R., Kurosaki, Y., Higaki, K., Miyoshi, S. I., Chang, K. S., & Kim, H. S. (2019). Pharmacokinetic analysis of new synthetic antimalarial N-251. Tropical medicine and health, 4740. https://doi.org/10.1186/s41182-019-0167-4
Okada, Kazuaki, et al. "Pharmacokinetic analysis of new synthetic antimalarial N-251." Tropical medicine and health vol. 47 (2019): 40. doi: https://doi.org/10.1186/s41182-019-0167-4
Okada K, Sato A, Hiramoto A, Isogawa R, Kurosaki Y, Higaki K, Miyoshi SI, Chang KS, Kim HS. Pharmacokinetic analysis of new synthetic antimalarial N-251. Trop Med Health. 2019 Jul 05;47:40. doi: 10.1186/s41182-019-0167-4. eCollection 2019. PMID: 31312098; PMCID: PMC6611044.
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Trop Med Health. 2019 Jul 05;47:40. doi: 10.1186/s41182-019-0167-4. eCollection 2019.

Pharmacokinetic analysis of new synthetic antimalarial N-251.

Tropical medicine and health

Kazuaki Okada, Akira Sato, Akiko Hiramoto, Rena Isogawa, Yuji Kurosaki, Kazutaka Higaki, Shin-Ichi Miyoshi, Kyung-Soo Chang, Hye-Sook Kim

Affiliations

  1. 1Division of International Infectious Diseases Control, Faculty of Pharmaceutical Sciences, Okayama University, 1-1-1 Tsushima-Naka, Kita-Ku, Okayama, Okayama 700-8530 Japan.
  2. 2Department of Biochemistry, Faculty of Pharmaceutical Sciences, Tokyo University of Science, 2641 Yamazaki, Noda, Chiba, 278-8510 Japan.
  3. 3Department of Pharmaceutical Formulation Design, Faculty of Pharmaceutical Sciences, Okayama University, 1-1-1 Tsushima-Naka, Kita-Ku, Okayama, Okayama 700-8530 Japan.
  4. 4Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, Okayama University, 1-1-1 Tsushima-Naka, Kita-Ku, Okayama, Okayama 700-8530 Japan.
  5. 5Department of Sanitary Microbiology, Faculty of Pharmaceutical Sciences, Okayama University, 1-1-1 Tsushima-Naka, Kita-Ku, Okayama, Okayama 700-8530 Japan.
  6. 6Department of Clinical Laboratory Science, College of Health Sciences, Catholic University of Pusan, Busan, 46252 Republic of Korea.

PMID: 31312098 PMCID: PMC6611044 DOI: 10.1186/s41182-019-0167-4

Abstract

BACKGROUND: With the emergence and growing number of drug-resistant

RESULTS: PK study of N-251 after intravenous and oral administration in mice showed plasma concentration of N-251 was decreased drastically by intravenous route.

CONCLUSIONS: N-251 has been selected as a potent antimalarial candidate. We found that N-251 showed short half-life in plasma, and AUCs increased proportionally to dose. With multiple doses of N-251, the plasma level of N-251 was greater than 10 ng/mL in normal-fed mice, and accumulation of N-251 was not observed; however, multiple treatments with N-251 are required for the complete cure of parasite-infected mice. Determining the appropriate dosage was an important step in the clinical applications of N-251.

Keywords: 6-(1,2,6,7-tetraoxaspiro [7.11] nonadec-4-yl)hexan-1-ol (N-251); Antimalarial medicine; Bioavailability (F); Pharmacokinetic (PK) study; Synthetic endoperoxide

Conflict of interest statement

Competing interestsThe authors declare that they have no competing interests.

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