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Delivery of antihuman African trypanosomiasis drugs across the blood-brain and blood-CSF barriers.
Adv Pharmacol. 2014; 71:245-75.AP

Abstract

Human African trypanosomiasis (HAT or sleeping sickness) is a potentially fatal disease caused by the parasite, Trypanosoma brucei sp. The parasites are transmitted by the bite of insect vectors belonging to the genus Glossina (tsetse flies) and display a life cycle strategy that is equally spread between human and insect hosts. T.b. gambiense is found in western and central Africa whereas, T.b. rhodesiense is found in eastern and southern Africa. The disease has two clinical stages: a blood stage after the bite of an infected tsetse fly, followed by a central nervous system (CNS) stage where the parasite penetrates the brain; causing death if left untreated. The blood-brain barrier (BBB) makes the CNS stage difficult to treat because it prevents 98% of all known compounds from entering the brain, including some anti-HAT drugs. Those that do enter the brain are toxic compounds in their own right and have serious side effects. There are only a few drugs available to treat HAT and those that do are stage specific. This review summarizes the incidence, diagnosis, and treatment of HAT and provides a close examination of the BBB transport of anti-HAT drugs and an overview of the latest drugs in development.

Authors+Show Affiliations

King's College London, Institute of Pharmaceutical Sciences, London, United Kingdom.King's College London, Institute of Pharmaceutical Sciences, London, United Kingdom.King's College London, Institute of Pharmaceutical Sciences, London, United Kingdom.King's College London, Institute of Pharmaceutical Sciences, London, United Kingdom.King's College London, Institute of Pharmaceutical Sciences, London, United Kingdom. Electronic address: sarah.thomas@kcl.ac.uk.

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't
Review

Language

eng

PubMed ID

25307219

Citation

Sekhar, Gayathri N., et al. "Delivery of Antihuman African Trypanosomiasis Drugs Across the Blood-brain and blood-CSF Barriers." Advances in Pharmacology (San Diego, Calif.), vol. 71, 2014, pp. 245-75.
Sekhar GN, Watson CP, Fidanboylu M, et al. Delivery of antihuman African trypanosomiasis drugs across the blood-brain and blood-CSF barriers. Adv Pharmacol. 2014;71:245-75.
Sekhar, G. N., Watson, C. P., Fidanboylu, M., Sanderson, L., & Thomas, S. A. (2014). Delivery of antihuman African trypanosomiasis drugs across the blood-brain and blood-CSF barriers. Advances in Pharmacology (San Diego, Calif.), 71, 245-75. https://doi.org/10.1016/bs.apha.2014.06.003
Sekhar GN, et al. Delivery of Antihuman African Trypanosomiasis Drugs Across the Blood-brain and blood-CSF Barriers. Adv Pharmacol. 2014;71:245-75. PubMed PMID: 25307219.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Delivery of antihuman African trypanosomiasis drugs across the blood-brain and blood-CSF barriers. AU - Sekhar,Gayathri N, AU - Watson,Christopher P, AU - Fidanboylu,Mehmet, AU - Sanderson,Lisa, AU - Thomas,Sarah A, Y1 - 2014/08/22/ PY - 2014/10/14/entrez PY - 2014/10/14/pubmed PY - 2015/6/17/medline KW - Blood–brain barrier KW - Breast cancer resistance protein KW - Eflornithine KW - Human African trypanosomiasis KW - Melarsoprol KW - Multidrug resistance-associated protein KW - Nifurtumox KW - P-glycoprotein KW - Pentamidine KW - Suramin SP - 245 EP - 75 JF - Advances in pharmacology (San Diego, Calif.) JO - Adv Pharmacol VL - 71 N2 - Human African trypanosomiasis (HAT or sleeping sickness) is a potentially fatal disease caused by the parasite, Trypanosoma brucei sp. The parasites are transmitted by the bite of insect vectors belonging to the genus Glossina (tsetse flies) and display a life cycle strategy that is equally spread between human and insect hosts. T.b. gambiense is found in western and central Africa whereas, T.b. rhodesiense is found in eastern and southern Africa. The disease has two clinical stages: a blood stage after the bite of an infected tsetse fly, followed by a central nervous system (CNS) stage where the parasite penetrates the brain; causing death if left untreated. The blood-brain barrier (BBB) makes the CNS stage difficult to treat because it prevents 98% of all known compounds from entering the brain, including some anti-HAT drugs. Those that do enter the brain are toxic compounds in their own right and have serious side effects. There are only a few drugs available to treat HAT and those that do are stage specific. This review summarizes the incidence, diagnosis, and treatment of HAT and provides a close examination of the BBB transport of anti-HAT drugs and an overview of the latest drugs in development. SN - 1557-8925 UR - https://www.unboundmedicine.com/medline/citation/25307219/Delivery_of_antihuman_African_trypanosomiasis_drugs_across_the_blood_brain_and_blood_CSF_barriers_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S1054-3589(14)00004-0 DB - PRIME DP - Unbound Medicine ER -