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Article: Using Cryopreserved

Jiménez-Díaz, María-Belén / Möhrle, Jörg J / Angulo-Barturen, Iñigo / Demarta-Gatsi, Claudia

2023 Volume 11, Issue 9

Abstract: In addition to vector control, long-lasting insecticidal nets and case management, the prevention of infection through vaccination and/or chemoprevention are playing an increasing role in the drive to eradicate malaria. These preventative approaches ... ...

Abstract	In addition to vector control, long-lasting insecticidal nets and case management, the prevention of infection through vaccination and/or chemoprevention are playing an increasing role in the drive to eradicate malaria. These preventative approaches represent opportunities for improvement: new drugs may be discovered that target the early infectious stages of the
Language	English
Publishing date	2023-08-31
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	2720891-6
ISSN	2076-2607
ISSN	2076-2607
DOI	10.3390/microorganisms11092209
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Article ; Online: Pharmacokinetic / pharmacodynamic relationships of liposomal amphotericin B and miltefosine in experimental visceral leishmaniasis.

Voak, Andrew A / Harris, Andy / Coteron-Lopez, Jose Miguel / Angulo-Barturen, Iñigo / Ferrer-Bazaga, Santiago / Croft, Simon L / Seifert, Karin

PLoS neglected tropical diseases

2021 Volume 15, Issue 3, Page(s) e0009013

Abstract: Background: There is a continued need to develop effective and safe treatments for visceral leishmaniasis (VL). Preclinical studies on pharmacokinetics and pharmacodynamics of anti-infective agents, such as anti-bacterials and anti-fungals, have ... ...

Abstract	Background: There is a continued need to develop effective and safe treatments for visceral leishmaniasis (VL). Preclinical studies on pharmacokinetics and pharmacodynamics of anti-infective agents, such as anti-bacterials and anti-fungals, have provided valuable information in the development and dosing of these agents. The aim of this study was to characterise the pharmacokinetic and pharmacodynamic properties of the anti-leishmanial drugs AmBisome and miltefosine in a preclinical disease model of VL. Methodology / principal findings: BALB/c mice were infected with L. donovani (MHOM/ET/67/HU3) amastigotes. Groups of mice were treated with miltefosine (orally, multi-dose regimen) or AmBisome (intravenously, single dose regimen) or left untreated as control groups. At set time points groups of mice were killed and plasma, livers and spleens harvested. For pharmacodynamics the hepatic parasite burden was determined microscopically from tissue impression smears. For pharmacokinetics drug concentrations were measured in plasma and whole tissue homogenates by LC-MS. Unbound drug concentrations were determined by rapid equilibrium dialysis. Doses exerting maximum anti-leishmanial effects were 40 mg/kg for AmBisome and 150 mg/kg (cumulatively) for miltefosine. AmBisome displayed a wider therapeutic range than miltefosine. Dose fractionation at a total dose of 2.5 mg/kg pointed towards concentration-dependent anti-leishmanial activity of AmBisome, favouring the administration of large doses infrequently. Protein binding was >99% for miltefosine and amphotericin B in plasma and tissue homogenates. Conclusion / significance: Using a PK/PD approach we propose optimal dosing strategies for AmBisome. Additionally, we describe pharmacokinetic and pharmacodynamic properties of miltefosine and compare our findings in a preclinical disease model to available knowledge from studies in humans. This approach also presents a strategy for improved use of animal models in the drug development process for VL.
MeSH term(s)	Amphotericin B/pharmacokinetics ; Amphotericin B/therapeutic use ; Animals ; Antiprotozoal Agents/pharmacokinetics ; Antiprotozoal Agents/therapeutic use ; Drug Therapy, Combination ; Homeodomain Proteins/genetics ; Humans ; Leishmaniasis, Visceral/drug therapy ; Liver/parasitology ; Male ; Mice ; Mice, Inbred BALB C ; Mice, Knockout ; Parasite Load ; Phosphorylcholine/analogs & derivatives ; Phosphorylcholine/pharmacokinetics ; Phosphorylcholine/therapeutic use ; Protein Binding/physiology
Chemical Substances	Antiprotozoal Agents ; Homeodomain Proteins ; liposomal amphotericin B ; Phosphorylcholine (107-73-3) ; RAG-1 protein (128559-51-3) ; miltefosine (53EY29W7EC) ; Amphotericin B (7XU7A7DROE)
Language	English
Publishing date	2021-03-02
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	2429704-5
ISSN	1935-2735 ; 1935-2727
ISSN (online)	1935-2735
ISSN	1935-2727
DOI	10.1371/journal.pntd.0009013
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Article ; Online: Humanised models of infection in the evaluation of anti-malarial drugs.

Angulo-Barturen, Iñigo / Ferrer, Santiago

Drug discovery today. Technologies

2013 Volume 10, Issue 3, Page(s) e351–7

Abstract: Humanised mice have a crucial role for drug discovery in malaria, which is the most important parasitic disease in the world and is caused by protozoa of the genus Plasmodium that selectively infect human hepatocytes and erythrocytes. There are currently ...

Abstract	Humanised mice have a crucial role for drug discovery in malaria, which is the most important parasitic disease in the world and is caused by protozoa of the genus Plasmodium that selectively infect human hepatocytes and erythrocytes. There are currently reliable humanised murine models for hepatic and erythrocytic stages of Plasmodium falciparum, which is the most pathogenic malarial species. These models are useful in the evaluation of drugs for malaria prevention and treatment, notably in exploiting the thousands of antimalarial hits discovered. The development of a humanised model for Plasmodium vivax and the validation of the P. falciparum models to inform optimal clinical studies are the next key goals to be achieved.
MeSH term(s)	Animals ; Antimalarials/therapeutic use ; Disease Models, Animal ; Drug Discovery ; Humans ; Malaria/drug therapy
Chemical Substances	Antimalarials
Language	English
Publishing date	2013-09
Publishing country	England
Document type	Journal Article ; Review
ISSN	1740-6749
ISSN (online)	1740-6749
DOI	10.1016/j.ddtec.2012.07.003
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Article ; Online: Macrocyclic Peptidomimetic Plasmepsin X Inhibitors with Potent

Kovada, Vadims / Withers-Martinez, Chrislaine / Bobrovs, Raitis / Ce Rule, Hele Na / Liepins, Edgars / Grinberga, Solveiga / Hackett, Fiona / Collins, Christine R / Kreicberga, Agrita / Jiménez-Díaz, María Belén / Angulo-Barturen, Iñigo / Rasina, Dace / Suna, Edgars / Jaudzems, Kristaps / Blackman, Michael J / Jirgensons, Aigars

Journal of medicinal chemistry

2023 Volume 66, Issue 15, Page(s) 10658–10680

Abstract: ... ...

Abstract	The
MeSH term(s)	Mice ; Animals ; Antimalarials/pharmacology ; Antimalarials/metabolism ; Peptidomimetics/pharmacology ; Peptidomimetics/metabolism ; Protease Inhibitors/pharmacology ; Protease Inhibitors/metabolism ; Aspartic Acid Endopeptidases ; Plasmodium falciparum/metabolism ; Protozoan Proteins
Chemical Substances	Antimalarials ; plasmepsin (EC 3.4.23.38) ; Peptidomimetics ; Protease Inhibitors ; Aspartic Acid Endopeptidases (EC 3.4.23.-) ; Protozoan Proteins
Language	English
Publishing date	2023-07-28
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	218133-2
ISSN	1520-4804 ; 0022-2623
ISSN (online)	1520-4804
ISSN	0022-2623
DOI	10.1021/acs.jmedchem.3c00812
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Article ; Online: Pharmacokinetic-pharmacodynamic and dose-response relationships of antituberculosis drugs: recommendations and standards for industry and academia.

Gumbo, Tawanda / Angulo-Barturen, Iñigo / Ferrer-Bazaga, Santiago

The Journal of infectious diseases

2015 Volume 211 Suppl 3, Page(s) S96–S106

Abstract: Background: Antimicrobial pharmacokinetic-pharmacodynamic (PK/PD) science is vital to early antibiotic drug development to enable more efficient dose-effect study designs, identification of doses that may suppress drug resistance and choice of ... ...

Abstract	Background: Antimicrobial pharmacokinetic-pharmacodynamic (PK/PD) science is vital to early antibiotic drug development to enable more efficient dose-effect study designs, identification of doses that may suppress drug resistance and choice of susceptibility breakpoints. Proper conduct of such studies is essential in the field of tuberculosis. Methods: We conducted an exhaustive review of literature on the hollow fiber system (HFS) model, murine model, and guinea pig model of tuberculosis as well as clinical studies to identify PK/PD studies that have been applied to antituberculosis therapy. Lessons learned are presented as recommendations and standards for both industry and academia in the field of antituberculosis drug development. Results: PK/PD studies have been performed for both first-line and experimental antituberculosis agents. When properly designed exposure-effect and dose-fractionation studies have been performed in preclinical models, optimal drug exposures, and PK/PD parameters identified in these models have been found to be similar to clinical studies. Susceptibility breakpoints identified using these methods differed from previous concentrations in the literature but were found to be similar to those in prospective clinical studies. Conclusions: Preclinical PK/PD studies are essential value added in the development of antituberculosis agents. We provide 8 recommendations and standards for the proper conduct of such studies.
MeSH term(s)	Animals ; Antitubercular Agents/pharmacokinetics ; Antitubercular Agents/pharmacology ; Clinical Trials as Topic ; Drug Evaluation, Preclinical ; Humans ; Tuberculosis/drug therapy
Chemical Substances	Antitubercular Agents
Language	English
Publishing date	2015-06-15
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't ; Review
ZDB-ID	3019-3
ISSN	1537-6613 ; 0022-1899
ISSN (online)	1537-6613
ISSN	0022-1899
DOI	10.1093/infdis/jiu610
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Article ; Online: Predicting Optimal Antimalarial Drug Combinations from a Standardized Plasmodium falciparum Humanized Mouse Model.

Antimicrobial agents and chemotherapy

2023 Volume 67, Issue 6, Page(s) e0157422

Abstract: The development of new combinations of antimalarial drugs is urgently needed to prevent the spread of parasites resistant to drugs in clinical use and contribute to the control and eradication of malaria. In this work, we evaluated a standardized ... ...

Abstract	The development of new combinations of antimalarial drugs is urgently needed to prevent the spread of parasites resistant to drugs in clinical use and contribute to the control and eradication of malaria. In this work, we evaluated a standardized humanized mouse model of erythrocyte asexual stages of Plasmodium falciparum (PfalcHuMouse) for the selection of optimal drug combinations. First, we showed that the replication of P. falciparum was robust and highly reproducible in the PfalcHuMouse model by retrospective analysis of historical data. Second, we compared the relative value of parasite clearance from blood, parasite regrowth after suboptimal treatment (recrudescence), and cure as variables of therapeutic response to measure the contributions of partner drugs to combinations
MeSH term(s)	Animals ; Mice ; Antimalarials/pharmacology ; Antimalarials/therapeutic use ; Plasmodium falciparum ; Retrospective Studies ; Peroxides ; Malaria, Falciparum/drug therapy ; Malaria, Falciparum/parasitology ; Drug Combinations
Chemical Substances	Antimalarials ; artefenomel (RIK029813G) ; Peroxides ; Drug Combinations
Language	English
Publishing date	2023-05-03
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	217602-6
ISSN	1098-6596 ; 0066-4804
ISSN (online)	1098-6596
ISSN	0066-4804
DOI	10.1128/aac.01574-22
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Article ; Online: Enzyme Therapy: Current Challenges and Future Perspectives.

de la Fuente, Miguel / Lombardero, Laura / Gómez-González, Alfonso / Solari, Cristina / Angulo-Barturen, Iñigo / Acera, Arantxa / Vecino, Elena / Astigarraga, Egoitz / Barreda-Gómez, Gabriel

International journal of molecular sciences

2021 Volume 22, Issue 17

Abstract: In recent years, enzymes have risen as promising therapeutic tools for different pathologies, from metabolic deficiencies, such as fibrosis conditions, ocular pathologies or joint problems, to cancer or cardiovascular diseases. Treatments based on the ... ...

Abstract	In recent years, enzymes have risen as promising therapeutic tools for different pathologies, from metabolic deficiencies, such as fibrosis conditions, ocular pathologies or joint problems, to cancer or cardiovascular diseases. Treatments based on the catalytic activity of enzymes are able to convert a wide range of target molecules to restore the correct physiological metabolism. These treatments present several advantages compared to established therapeutic approaches thanks to their affinity and specificity properties. However, enzymes present some challenges, such as short in vivo half-life, lack of targeted action and, in particular, patient immune system reaction against the enzyme. For this reason, it is important to monitor serum immune response during treatment. This can be achieved by conventional techniques (ELISA) but also by new promising tools such as microarrays. These assays have gained popularity due to their high-throughput analysis capacity, their simplicity, and their potential to monitor the immune response of patients during enzyme therapies. In this growing field, research is still ongoing to solve current health problems such as COVID-19. Currently, promising therapeutic alternatives using the angiotensin-converting enzyme 2 (ACE2) are being studied to treat COVID-19.
MeSH term(s)	Angiotensin-Converting Enzyme 2/pharmacology ; Angiotensin-Converting Enzyme 2/therapeutic use ; COVID-19/drug therapy ; Clinical Trials, Phase II as Topic ; Drug Compounding/methods ; Enzyme Stability ; Enzyme Therapy/history ; Enzyme Therapy/methods ; Enzyme Therapy/trends ; Half-Life ; History, 20th Century ; History, 21st Century ; Humans ; Recombinant Proteins/pharmacology ; Recombinant Proteins/therapeutic use ; SARS-CoV-2/drug effects ; SARS-CoV-2/metabolism ; Treatment Outcome ; Virus Internalization/drug effects
Chemical Substances	Recombinant Proteins ; Angiotensin-Converting Enzyme 2 (EC 3.4.17.23) ; alunacedase alfa (FA2I4Z873U)
Language	English
Publishing date	2021-08-25
Publishing country	Switzerland
Document type	Historical Article ; Journal Article ; Review
ZDB-ID	2019364-6
ISSN	1422-0067 ; 1422-0067 ; 1661-6596
ISSN (online)	1422-0067
ISSN	1422-0067 ; 1661-6596
DOI	10.3390/ijms22179181
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Article ; Online: Chemoprotective Antimalarial Activity of P218 against Plasmodium falciparum: A Randomized, Placebo-Controlled Volunteer Infection Study.

Chughlay, Mohamed Farouk / El Gaaloul, Myriam / Donini, Cristina / Campo, Brice / Berghmans, Pieter-Jan / Lucardie, Alexander / Marx, Michael W / Cherkaoui-Rbati, Mohammed H / Langdon, Grant / Angulo-Barturen, Iñigo / Viera, Sara / Rosanas-Urgell, Anna / Van Geertruyden, Jean-Pierre / Chalon, Stephan

The American journal of tropical medicine and hygiene

2021 Volume 104, Issue 4, Page(s) 1348–1358

Abstract: P218 is a highly selective dihydrofolate reductase inhibitor with potent in vitro activity against pyrimethamine-resistant Plasmodium falciparum. This single-center, randomized, double-blind, placebo-controlled phase Ib study evaluated P218 safety, ... ...

Abstract	P218 is a highly selective dihydrofolate reductase inhibitor with potent in vitro activity against pyrimethamine-resistant Plasmodium falciparum. This single-center, randomized, double-blind, placebo-controlled phase Ib study evaluated P218 safety, pharmacokinetics, and chemoprotective efficacy in a P. falciparum sporozoite (PfSPZ) volunteer infection study (VIS). Consecutive dose safety and tolerability were evaluated (cohort 1), with participants receiving two oral doses of P218 1,000 mg 48 hours apart (n = 6), or placebo (n = 2). P218 chemoprotective efficacy was assessed (cohorts 2 and 3) with direct venous inoculation of 3,200 aseptic, cryopreserved PfSPZ (NF54 strain) followed 2 hours later with two P218 doses of 1,000 mg (cohort 2, n = 9) or 100 mg (cohort 3, n = 9) administered 48 hours apart, or placebo (n = 6). Parasitemia was assessed from day 7 using quantitative PCR targeting the var gene acidic terminal sequence (varATS qPCR). By day 28, all participants in cohort 2 (P218 1,000 mg) and 8/9 in cohort 3 (P218 100 mg) were sterilely protected post-PfSPZ VIS, confirming P218 P. falciparum chemoprotective activity. With placebo, all six participants became parasitemic (geometric mean time to positive parasitemia 10.6 days [90% CI: 9.9-11.4]). P218 pharmacokinetics were similar in participants with or without induced infection. Adverse events of any cause occurred in 45.8% (11/24) of participants who received P218 and 50.0% (4/8) following placebo; all were mild/moderate in severity, transient, and self-limiting. There were no clinically relevant changes in laboratory parameters, vital signs, or electrocardiograms. P218 displayed excellent chemoprotective efficacy against P. falciparum with favorable safety and tolerability.
Language	English
Publishing date	2021-02-08
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	2942-7
ISSN	1476-1645 ; 0002-9637
ISSN (online)	1476-1645
ISSN	0002-9637
DOI	10.4269/ajtmh.20-1165
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Article: Study of Tissue-Specific Reactive Oxygen Species Formation by Cell Membrane Microarrays for the Characterization of Bioactive Compounds.

Elexpe, Ane / Nieto, Nerea / Fernández-Cuétara, Claudia / Domínguez-Fernández, Celtia / Morera-Herreras, Teresa / Torrecilla, María / Miguélez, Cristina / Laso, Antonio / Ochoa, Eneko / Bailen, María / González-Coloma, Azucena / Angulo-Barturen, Iñigo / Astigarraga, Egoitz / Barreda-Gómez, Gabriel

Membranes

2021 Volume 11, Issue 12

Abstract: The production of reactive oxygen species (ROS) increases considerably in situations of cellular stress, inducing lipid peroxidation and multiple alterations in proteins and nucleic acids. However, sensitivity to oxidative damage varies between organs ... ...

Abstract	The production of reactive oxygen species (ROS) increases considerably in situations of cellular stress, inducing lipid peroxidation and multiple alterations in proteins and nucleic acids. However, sensitivity to oxidative damage varies between organs and tissues depending on the triggering process. Certain drugs used in the treatment of diverse diseases such as malaria have side effects similar to those produced by oxidative damage, although no specific study has been conducted. For this purpose, cell membrane microarrays were developed and the superoxide production evoked by the mitochondrial activity was assayed in the presence of specific inhibitors: rotenone, antimycin A and azide. Once the protocol was set up on cell membrane isolated from rat brain areas, the effect of six antimalarial drugs (atovaquone, quinidine, doxycycline, mefloquine, artemisinin, and tafenoquine) and two essential oils (
Language	English
Publishing date	2021-11-29
Publishing country	Switzerland
Document type	Journal Article
ISSN	2077-0375
ISSN	2077-0375
DOI	10.3390/membranes11120943
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Article: Determination of the Pharmacokinetics and Pharmacodynamics of Isoniazid, Rifampicin, Pyrazinamide and Ethambutol in a Cross-Over Cynomolgus Macaque Model of

Pharmaceutics

2022 Volume 14, Issue 12

Abstract: Innovative cross-over study designs were explored in non-human primate (NHP) studies to determine the value of this approach for the evaluation of drug efficacy against tuberculosis (TB). Firstly, the pharmacokinetics (PK) of each of the drugs Isoniazid ( ...

Abstract	Innovative cross-over study designs were explored in non-human primate (NHP) studies to determine the value of this approach for the evaluation of drug efficacy against tuberculosis (TB). Firstly, the pharmacokinetics (PK) of each of the drugs Isoniazid (H), Rifampicin (R), Pyrazinamide (Z) and Ethambutol (E), that are standardly used for the treatment of tuberculosis, was established in the blood of macaques after oral dosing as a monotherapy or in combination. Two studies were conducted to evaluate the pharmacokinetics and pharmacodynamics of different drug combinations using cross-over designs. The first employed a balanced, three-period Pigeon design with an extra period; this ensured that treatment by period interactions and carry-over could be detected comparing the treatments HR, HZ and HRZ using H37Rv as the challenge strain of
Language	English
Publishing date	2022-11-30
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	2527217-2
ISSN	1999-4923
ISSN	1999-4923
DOI	10.3390/pharmaceutics14122666
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