IP Library Granted Patent US 12,433,869
Granted Patent B2
US 12,433,869 · App. 17/605,025 · Granted Oct 7, 2025

Preventing and treating malaria

Inventors: Ian Basil Shine (Swampscott, MA); Thomas Adam Shine (Brookline, MA)
Assignees: Ian Basil Shine; Thomas Adam Shine
A61K31/4045A61K31/405A61K45/06A61P33/06C12N5/0641G01N33/5091G01N2333/445
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Quick Facts
Patent No.
US 12,433,869
App. No.
17/605,025
Granted
Oct 7, 2025
Kind
B2
Abstract

Methods of treating and preventing malaria infection, comprising administering a therapeutically effective amount of cell permeability modulating therapy are provided herein. Among other things, the present disclosure provides parameters that define subjects who are relatively susceptible or resistant to malaria infection. The present disclosure also provides therapeutic strategies for increasing malarial resistance and/or imparting a resistant state on subjects.

Claims (31)

1. A method of treating or preventing malaria, comprising administering to a subject in need thereof red blood cell (RBC) permeability modulating therapy.

2. The method of claim 1 , wherein the RBC permeability modulating therapy is or comprises administering a therapeutically effective amount of a RBC permeability modulating agent.

3. The method of claim 2 , wherein the RBC permeability modulating agent is 5-hydroxytryptamine, or a pharmaceutically acceptable salt thereof, and

wherein the RBC permeability modulating therapy comprises administering the RBC permeability modulating agent to the subject at a concentration in a range from about 500 ng/ml to about 900 ng/mL.

4. The method of claim 2 , wherein the RBC permeability modulating agent comprises 5-hydroxytryptophan (5-HTP).

5. The method of claim 2 , wherein the RBC permeability modulating agent is or comprises a serotonin norepinephrine reuptake inhibitor (SNRI), monoamine oxidase inhibitors (MAOI), tricyclic antidepressants (TCA), or serotonin antagonist and reuptake inhibitor (SARI).

6. The method of claim 2 , wherein the RBC permeability modulating agent is administered orally in an oral dosage form.

7. The method of claim 1 , wherein the subject has a PKO from about 120 mOsm/kg to about 185 mOsm/kg, from about 130 mOsm/kg to about 160 mOsm/kg, from about 130 mOsm/kg to about 150 mOsm/kg, from about 132 mOsm/kg to about 148 mOsm/kg, from about 135 mOsm/kg to about 145 mOsm/kg, or from about 138 mOsm/kg to about 142 mOsm/kg.

8. The method of claim 1 , wherein the subject has received or is receiving one or more additional agents selected from mefloquine, doxycycline, atovaquone, and proguanil.

9. The method of claim 1 , wherein the subject has received or is receiving one or more additional agents selected from amodiaquine, arteether, artemether, artesunate, artemisinin, atovaquone, chloroquine, cinchoine, cinchonidine, clindamycin, dihydroartemisinin, doxycycline, halofantrine, hydroxychloroquine, lumefantrine, mefloquine, piperaquine, primaquine, pyrimethamine, quinidine, quinine, sulfadoxine, sulfamethoxypyridazine, tafenoquine, and tetracycline.

10. The method of claim 1 , wherein the subject is resistant to treatment with one or more agents selected from amodiaquine, arteether, artemether, artesunate, artemisinin, atovaquone, chloroquine, cinchoine, cinchonidine, clindamycin, dihydroartemisinin, doxycycline, halofantrine, hydroxychloroquine, lumefantrine, mefloquine, piperaquine, primaquine, pyrimethamine, quinidine, quinine, sulfadoxine, sulfamethoxypyridazine, tafenoquine, and tetracycline.

11. The method of claim 1 , wherein the subject has one or more of the following risk factors:

(i) lives in a geographical area with a high incidence of malaria;

(ii) has recently traveled to a geographical area with a high incidence of malaria;

(iii) has recently been bitten by a mosquito in a geographical area with a high incidence of malaria;

(iv) is harboring dormant malaria parasite;

(v) under 5 years of age; or

(vi) is pregnant.

12. The method of claim 2 , wherein the RBC permeability modulating agent decreases the RBC permeability of the subject.

13. The method of claim 2 , wherein the RBC permeability modulating agent comprises lactose, and

wherein the RBC permeability modulating therapy comprises administering the RBC permeability modulating agent to the subject at a concentration of about 1:20 (v/v) in saturated lactose solution.

14. The method of claim 2 , wherein the RBC permeability modulating agent comprises amphotericin B, and

wherein the RBC permeability modulating agent is administered to the subject at a concentration of about 0.5 μg/mL.

15. The method of claim 2 , the method further comprising:

establishing a baseline cell membrane permeability parameter of the subject, the cell membrane permeability parameter comprising Pk0; and

administering the RBC permeability modulating agent to the subject at a regular interval until the cell membrane permeability parameter of the subject decreases by a predetermined amount compared to the baseline cell membrane permeability parameter of the subject.

16. The method of claim 15 , wherein the RBC permeability modulating agent comprises at least one of amphotericin B, lactose, and 5-hydroxytryptamine.

17. The method of claim 16 , wherein the predetermined amount comprises a decrease in Pk0 in range from about 20 mOsm/kg to about 30 mOsm/kg.

18. The method of claim 17 , comprising preventing malaria, wherein administering the RBC permeability modulating agent to the subject occurs prior to exposure of the subject to malaria.

19. The method of claim 17 , comprising treating malaria, wherein administering the RBC permeability modulating agent to the subject occurs after exposure of the subject to malaria.

20. The method of claim 16 , wherein the predetermined amount comprises a decrease to a Pk0 value below about 120 mOsm/kg.

Continuity (3)
Provisional Application 62943689 · Dec 4, 2019
Provisional Application 62836997 · Apr 22, 2019
Related Publication 20220211670A1 · Jul 7, 2022
References Cited (42)
US 4159895A · Shine · 1979 [cited by applicant]
US 4278936A · Shine · 1981 [cited by applicant]
US 6086918A · Stern et al. · 2000 [cited by applicant]
US 6673574B2 · Stern et al. · 2004 [cited by applicant]
US 6960355B2 · Leone-Bay et al. · 2005 [cited by applicant]
US 7351741B2 · Weidner et al. · 2008 [cited by applicant]
US 20100278920A1 · Turos et al. · 2010 [cited by applicant]
WO WO1996004898A1 · 1996 [cited by applicant]
WO WO9724529A1 · 1997 [cited by applicant]
WO WO9724598A1 · 1997 [cited by applicant]
WO WO9724599A1 · 1997 [cited by applicant]
WO WO9724600A1 · 1997 [cited by applicant]
WO WO9724601A1 · 1997 [cited by applicant]
WO WO970024598 · 1997 [cited by examiner]
WO WO0039559A2 · 2000 [cited by applicant]
WO WO0039560A2 · 2000 [cited by applicant]
WO WO2007131286A1 · 2007 [cited by applicant]
WO WO2010011537A1 · 2010 [cited by applicant]
WO WO2020117983A1 · 2020 [cited by applicant]
WO WO2020219445A1 · 2020 [cited by applicant]
WO WO2021113652A1 · 2021 [cited by applicant]
Glushakova et al., Curr Biol 20(12) (2010) pp. 1117-1121. [cited by examiner]
Dennis et a. Amto, ocrpb Agemts Cje, ptjer. 2018, vol. 62(6) pp. 1-17. [cited by examiner]
Locher et al., Channel Antimicrob Agents Chemother, vol. 47(12) (2003) pp. 3806-3809. [cited by examiner]
Ginsburg et al., Biochim Biophys Acta (1983) vol. 729(1). [cited by examiner]
Khairul et al. Jpn J'nal Infect Dis (2006), vol. 59(5) pp. 329-331. [cited by examiner]
Beraldo, F.H. and Garcia, C.R.S., Products of tryptophan catabolisminduce Ca2+ release and modulate the cell cycle of Plasmodium falciparum malaria parasites, J. Pineal. Res., 39(3):224-230 (2005). [cited by applicant]
Bitonti, A.J. et al., Reversal of chloroquine resistance in malaria parasite Plasmodium falciparum by desipramine, Science, 242(4883):1301-1303 (1988). [cited by applicant]
Dutta, P. et al., Antimalarial properties of imipramine and amitriptyline, J. Protozool., 37(1):54-58 (1990). [cited by applicant]
Singh, N. and Puri, S.K., Modulation of halofantrine resistance after coadministration of halofantrine with diverse pharmacological agents in a rodent malaria model, Life Sci., 67(11):1345-1354 (2000). [cited by applicant]
Cooke, B.M. et al., Malaria and the red blood cell membrane, Semin. Hematol., 41(2):173-188 (2004). [cited by applicant]
Dennis et al., Cell Swelling Induced by the Antimalarial KAE609 (Cipargamin) and Other PfATP4-Associated Antimalarials, Antimicrob Agents Chemother, 62(6):1-17, (2008). [cited by applicant]
Diagne, N. et al., Incidence of clinical malaria in pregnant women exposed to intense perennial transmission, Transactions of the Royal Society of Tropical Medicine and Hygiene, 91(2):166-170 (1997). [cited by applicant]
Gilboa-Garber et al., Structural Specificity of Serotonin Effect on Human Erythrocyte Fragility, Mol Genet Metab., 64(4):283-285, (1998). [cited by applicant]
Ginsburg et al., Uptake of L-tryptophan by Erythrocytes Infected With Malaria Parasites ( [cited by applicant]
Glushakova et al., New Stages in the Program of Malaria Parasite Egress Imaged in Normal and Sickle Erythrocytes, Curr Biol, 20(12):1117-1121, (2010). [cited by applicant]
International Search Report for PCT/US2020/029114 filed Apr. 21, 2020, 5 pages, (Jul. 20, 2020). [cited by applicant]
Khairul et al., Fluoxetine Potentiates Chloroquine and Mefloquine Effect on Multidrug-Resistant Plasmodium Falciparum in Vitro, Jpn J Infect Dis, 59(5):329-331 (2006). [cited by applicant]
Locher et al., 5HT1A Serotonin Receptor Agonists Inhibit Plasmodium Falciparum by Blocking a Membrane Channel, Antimicrob Agents Chemother, 47(12):3806-3809, (2003). [cited by applicant]
Mohandas, N. and An, X., Malaria and Human Red Blood Cells, Med Microbiol Immunol., 201(4):593-598 (2012). [cited by applicant]
Saudek, C.D. et al., A preliminary trial of the programmable implantable medication system for insulin delivery, N. Engl. J. Med., 321(9):574-579 (1989). [cited by applicant]
Written Opinion for PCT/US2020/029114 filed Apr. 21, 2020, 5 pages, (Jul. 20, 2020). [cited by applicant]