Novel Small Molecule Antimalarials for Elimination of Malaria Transmission


The transmission of malaria begins with injection of sporozoites into a human from the bite of a female anopheles mosquito, which initiates the malarial life cycle in humans. When a mosquito bites an infected human, the ingested male and female malaria gametocytes fuse to form a zygote that eventually becomes an oocyst. Each oocyst produces thousands of sporozoites which migrate to the mosquito salivary glands, ready to infect a new human host.

Currently, the available therapeutics for malaria can effectively eliminate the asexual stages of malarial parasites that cause clinical symptoms in patients. However, their abilities to eliminate the gametocyte (sexual stage of the parasites) as well as the liver stage parasites are limited. The subject technology involves novel compounds, which include Torin 2, that are potently gametocytocidal in in vitro assays and in a mouse model of malaria, completely blocked the host-to-mosquito transmission by suppressing oocytes formation in mosquitoes.

Potential Commercial Applications: Competitive Advantages:
  • Novel therapeutics for elimination of malaria transmission and treatment of drug resistant malaria patients.
 
  • These novel compounds are effective against gametocytes, the sexual stage of malarial parasites, whereas currently available antimalarials have limited effectiveness against this form of the parasite.
  • The compounds provide an alternative treatment against malaria for patients with glucose-6-phosphate dehydrogenase deficiency.
  • These compounds are active against drug resistant strains of malaria.


Development Stage:
  • Early-stage
  • In vitro data available
  • In vivo data available (animal)


Inventors:

John McKew (NCATS)  ➽ more inventions...

Wei Zheng (NCATS)  ➽ more inventions...

Seameen Dehdashti (NCATS)  ➽ more inventions...

Noel Southall (NCATS)  ➽ more inventions...

Wenwei Huang (NCATS)  ➽ more inventions...

Wei Sun (NCATS)  ➽ more inventions...

Takeshi Tanaka (NIAID)  ➽ more inventions...


Intellectual Property:
US Application No. 15/036,355
US Application No. 61/904,884
PCT Application No. PCT/US2014/065671

Publications:
Sun W, et al. PMID 24434750

Licensing Contact:
Suryanarayana Vepa, Ph.D.
Email: sury.vepa@nih.gov
Phone: 301-217-9197

OTT Reference No: E-751-2013/0
Updated: Nov 18, 2015