Malaria medicines: a glass half full?

Malaria and the Millennium Development Goals

(2015) Stephen Owens   ARCHIVES OF DISEASE IN CHILDHOOD

Genetic architecture of artemisinin-resistant Plasmodium falciparum

(2015) Olivo Miotto et al.   NATURE GENETICS

Antimalarial 4(1H)-pyridones bind to the Qisite of cytochromebc1

(2015) Michael J. Capper et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Lysine Acetylation in Sexual Stage Malaria Parasites Is a Target for Antimalarial Small Molecules

(2014) Katharine Trenholme et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

First-in-Humans Study of the Safety, Tolerability, and Pharmacokinetics of ACT-451840, a New Chemical Entity with Antimalarial Activity

(2014) Shirin Bruderer et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Repurposing the Open Access Malaria Box To Discover Potent Inhibitors of Toxoplasma gondii and Entamoeba histolytica

(2014) Fabrice F. Boyom et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

A First-in-Human Randomized, Double-Blind, Placebo-Controlled, Single- and Multiple-Ascending Oral Dose Study of Novel Antimalarial Spiroindolone KAE609 (Cipargamin) To Assess Its Safety, Tolerability, and Pharmacokinetics in Healthy Adult Volunteers

(2014) F. Joel Leong et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Pharmacokinetic-Pharmacodynamic Analysis of Spiroindolone Analogs and KAE609 in a Murine Malaria Model

(2014) Suresh B. Lakshminarayana et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

KAF156 Is an Antimalarial Clinical Candidate with Potential for Use in Prophylaxis, Treatment, and Prevention of Disease Transmission

(2014) Kelli L. Kuhen et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Identification of Cryptosporidium parvum Active Chemical Series by Repurposing the Open Access Malaria Box

(2014) K. Bessoff et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Discovery of HDAC inhibitors with potent activity against multiple malaria parasite life cycle stages

(2014) Finn K. Hansen et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Physicochemical and drug metabolism characterization of a series of 4-aminoquinoline-3-hydroxypyridin-4-one hybrid molecules with antimalarial activity

(2014) Roslyn Thelingwani et al.   Expert Opinion on Drug Metabolism & Toxicology

Efficacy and Safety of Triple Combination Therapy With Artesunate-Amodiaquine–Methylene Blue for Falciparum Malaria in Children: A Randomized Controlled Trial in Burkina Faso

(2014) Boubacar Coulibaly et al.   JOURNAL OF INFECTIOUS DISEASES

Controlled Human Malaria Infection

(2014) M. Spring et al.   JOURNAL OF INFECTIOUS DISEASES

Fluorine Modulates Species Selectivity in the Triazolopyrimidine Class of Plasmodium falciparum Dihydroorotate Dehydrogenase Inhibitors

(2014) Xiaoyi Deng et al.   JOURNAL OF MEDICINAL CHEMISTRY

Identification of Plasmodium PI4 kinase as target of MMV390048 by chemoproteomics

(2014) Sonja Ghidelli-Disse et al.   MALARIA JOURNAL

Tafenoquine and NPC-1161B require CYP 2D metabolism for anti-malarial activity: implications for the 8-aminoquinoline class of anti-malarial compounds

(2014) Sean R Marcsisin et al.   MALARIA JOURNAL

Screening and hit evaluation of a chemical library against blood-stage Plasmodium falciparum

(2014) Vicky M Avery et al.   MALARIA JOURNAL

Investigation of Indolglyoxamide and Indolacetamide Analogues of Polyamines as Antimalarial and Antitrypanosomal Agents

(2014) Jiayi Wang et al.   Marine Drugs

Diverse chemotypes disrupt ion homeostasis in the malaria parasite

(2014) Adele M. Lehane et al.   MOLECULAR MICROBIOLOGY

Persistence and activation of malaria hypnozoites in long-term primary hepatocyte cultures

(2014) Laurent Dembélé et al.   NATURE MEDICINE

Next-generation antimalarial from phenotypic screen shows clinical promise

(2014) Megan Cully   NATURE REVIEWS DRUG DISCOVERY

Spread of Artemisinin Resistance in Plasmodium falciparum Malaria

(2014) Elizabeth A. Ashley et al.   NEW ENGLAND JOURNAL OF MEDICINE

Spiroindolone KAE609 for Falciparum and Vivax Malaria

(2014) Nicholas J. White et al.   NEW ENGLAND JOURNAL OF MEDICINE

Successful vaccines for naturally occurring protozoal diseases of animals should guide human vaccine research. A review of protozoal vaccines and their designs

(2014) MILTON M. MCALLISTER   PARASITOLOGY

Identification of MMV Malaria Box Inhibitors of Perkinsus marinus Using an ATP-Based Bioluminescence Assay

(2014) Yesmalie Alemán Resto et al.   PLoS One

(+)-SJ733, a clinical candidate for malaria that acts through ATP4 to induce rapid host-mediated clearance ofPlasmodium

(2014) María Belén Jiménez-Díaz et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

K13-propeller mutations confer artemisinin resistance in Plasmodium falciparum clinical isolates

(2014) J. Straimer et al.   SCIENCE

Plasmepsin Inhibitory Activity and Structure-Guided Optimization of a Potent Hydroxyethylamine-Based Antimalarial Hit

(2014) Kristaps Jaudzems et al.   ACS Medicinal Chemistry Letters

Pyrazoleamide compounds are potent antimalarials that target Na+ homeostasis in intraerythrocytic Plasmodium falciparum

(2014) Akhil B. Vaidya et al.   Nature Communications

Efficacy and Safety of the RTS,S/AS01 Malaria Vaccine during 18 Months after Vaccination: A Phase 3 Randomized, Controlled Trial in Children and Young Infants at 11 African Sites

(2014)   PLOS MEDICINE

Orally Active Antischistosomal Early Leads Identified from the Open Access Malaria Box

(2014) Katrin Ingram-Sieber et al.   PLoS Neglected Tropical Diseases

Recent advances in malaria drug discovery

(2013) Marco A. Biamonte et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

A Microscale Human Liver Platform that Supports the Hepatic Stages of Plasmodium falciparum and vivax

(2013) Sandra March et al.   Cell Host & Microbe

Na+ Regulation in the Malaria Parasite Plasmodium falciparum Involves the Cation ATPase PfATP4 and Is a Target of the Spiroindolone Antimalarials

(2013) Natalie J. Spillman et al.   Cell Host & Microbe

A Continuous-Flow Process for the Synthesis of Artemisinin

(2013) Daniel Kopetzki et al.   CHEMISTRY-A EUROPEAN JOURNAL

Models for open innovation in the pharmaceutical industry

(2013) Alexander Schuhmacher et al.   DRUG DISCOVERY TODAY

Antiparasitic effect of a fraction enriched in tight-binding protease inhibitors isolated from the Caribbean coral Plexaura homomalla

(2013) Emir Salas-Sarduy et al.   EXPERIMENTAL PARASITOLOGY

Tafenoquine plus chloroquine for the treatment and relapse prevention of Plasmodium vivax malaria (DETECTIVE): a multicentre, double-blind, randomised, phase 2b dose-selection study

(2013) Alejandro Llanos-Cuentas et al.   LANCET

Single-dose radical cure of Plasmodium vivax : a step closer

(2013) Ric N Price et al.   LANCET

Single low-dose primaquine to reduce malaria transmission

(2013) Richard W Steketee et al.   LANCET INFECTIOUS DISEASES

Triangular test design to evaluate tinidazole in the prevention of Plasmodium vivax relapse

(2013) Louis Macareo et al.   MALARIA JOURNAL

MMV in partnership: the Eurartesim® experience

(2013) David Ubben et al.   MALARIA JOURNAL

The economic costs of malaria in children in three sub-Saharan countries: Ghana, Tanzania and Kenya

(2013) Elisa Sicuri et al.   MALARIA JOURNAL

Designing the next generation of medicines for malaria control and eradication

(2013) Jeremy N Burrows et al.   MALARIA JOURNAL

Identification of inhibitors of Plasmodium falciparum gametocyte development

(2013) Sandra Duffy et al.   MALARIA JOURNAL

Targeting Plasmodium PI(4)K to eliminate malaria

(2013) Case W. McNamara et al.   NATURE

A molecular marker of artemisinin-resistant Plasmodium falciparum malaria

(2013) Frédéric Ariey et al.   NATURE

The GHIT fund shows its cards

(2013) David Holmes   NATURE REVIEWS DRUG DISCOVERY

European Lead Factory opens for business

(2013) Asher Mullard   NATURE REVIEWS DRUG DISCOVERY

Antimalarial drug discovery — approaches and progress towards new medicines

(2013) Erika L. Flannery et al.   NATURE REVIEWS MICROBIOLOGY

The antimalarial ferroquine: from bench to clinic

(2013) C. Biot et al.   Parasite

The Open Access Malaria Box: A Drug Discovery Catalyst for Neglected Diseases

(2013) Thomas Spangenberg et al.   PLoS One

Protection Against Malaria by Intravenous Immunization with a Nonreplicating Sporozoite Vaccine

(2013) R. A. Seder et al.   SCIENCE

Role of type-II pathway in apoptotic cell death induction by photosensitized CDRI-97/78 under ambient exposure of UV-B

(2013) Ashish Dwivedi et al.   TOXICOLOGY LETTERS

Evaluation of Aminohydantoins as a Novel Class of Antimalarial Agents

(2013) Marvin J. Meyers et al.   ACS Medicinal Chemistry Letters

The Global Health Innovative Technology (GHIT) Fund: financing medical innovations for neglected populations

(2013) BT Slingsby et al.   Lancet Global Health

Continuous-Flow Synthesis of the Anti-Malaria Drug Artemisinin

(2012) François Lévesque et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Inadequate Efficacy of a New Formulation of Fosmidomycin-Clindamycin Combination in Mozambican Children Less than Three Years Old with Uncomplicated Plasmodium falciparum Malaria

(2012) Miguel Lanaspa et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Pharmacokinetics of Ferroquine, a Novel 4-Aminoquinoline, in Asymptomatic Carriers of Plasmodium falciparum Infections

(2012) Christian Supan et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Antimalarial Activity of the Anticancer Histone Deacetylase Inhibitor SB939

(2012) Subathdrage D. M. Sumanadasa et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

MK-4815, a Potential New Oral Agent for Treatment of Malaria

(2012) Mary Ann Powles et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Reduced Artemisinin Susceptibility of Plasmodium falciparum Ring Stages in Western Cambodia

(2012) B. Witkowski et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Experimental human influenza: observations from studies of influenza antivirals

(2012) Frederick G Hayden   ANTIVIRAL THERAPY

Intersex Effect of Lamotrigine on the Pharmacokinetic Parameters of CDRI-97/78, a Novel Trioxane Antimalarial Compound, in Rats

(2012) H. Kushwaha et al.   ARZNEIMITTEL-FORSCHUNG-DRUG RESEARCH

Novel in vivo active anti-malarials based on a hydroxy-ethyl-amine scaffold

(2012) Claire-Lise Ciana et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Arterolane Maleate Plus Piperaquine Phosphate for Treatment of Uncomplicated Plasmodium falciparum Malaria: A Comparative, Multicenter, Randomized Clinical Trial

(2012) N. Valecha et al.   CLINICAL INFECTIOUS DISEASES

Adjuvants for human vaccines

(2012) Carl R Alving et al.   CURRENT OPINION IN IMMUNOLOGY

The Need for New Antimalarial Drugs Less Prone to Resistance

(2012) Harald Noedl   CURRENT PHARMACEUTICAL DESIGN

Exploration of 4(1H)-pyridones as a novel family of potent antimalarial inhibitors of the plasmodial cytochrome bc1

(2012) José M Bueno et al.   Future Medicinal Chemistry

Drug Screen Targeted at Plasmodium Liver Stages Identifies a Potent Multistage Antimalarial Drug

(2012) Filipa P. da Cruz et al.   JOURNAL OF INFECTIOUS DISEASES

3,5-Diaryl-2-aminopyridines as a Novel Class of Orally Active Antimalarials Demonstrating Single Dose Cure in Mice and Clinical Candidate Potential

(2012) Yassir Younis et al.   JOURNAL OF MEDICINAL CHEMISTRY

A Concise Synthesis of (+)-Artemisinin

(2012) Chunyin Zhu et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Emergence of artemisinin-resistant malaria on the western border of Thailand: a longitudinal study

(2012) Aung Pyae Phyo et al.   LANCET

Malaria resurgence: a systematic review and assessment of its causes

(2012) Justin M Cohen et al.   MALARIA JOURNAL

The global pipeline of new medicines for the control and elimination of malaria

(2012) Melinda P Anthony et al.   MALARIA JOURNAL

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(2012) Ian Copple et al.   MOLECULAR MEDICINE

Mosquito Feeding Assays to Determine the Infectiousness of Naturally Infected Plasmodium falciparum Gametocyte Carriers

(2012) Teun Bousema et al.   PLoS One

Malarial dihydrofolate reductase as a paradigm for drug development against a resistance-compromised target

(2012) Y. Yuthavong et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Experimentally induced blood stage malaria infection as a tool for clinical research

(2012) Christian R. Engwerda et al.   TRENDS IN PARASITOLOGY

A Chemical Genomic Analysis of Decoquinate, aPlasmodium falciparumCytochromebInhibitor

(2011) Tae-gyu Nam et al.   ACS Chemical Biology

Intermittent Treatment to Prevent Pregnancy Malaria Does Not Confer Benefit in an Area of Widespread Drug Resistance

(2011) W. E. Harrington et al.   CLINICAL INFECTIOUS DISEASES

Structure-Guided Lead Optimization of Triazolopyrimidine-Ring Substituents Identifies PotentPlasmodium falciparumDihydroorotate Dehydrogenase Inhibitors with Clinical Candidate Potential

(2011) Jose M. Coteron et al.   JOURNAL OF MEDICINAL CHEMISTRY

Natural products as starting points for future anti-malarial therapies: going back to our roots?

(2011) Timothy NC Wells   MALARIA JOURNAL

Phase I randomized dose-ascending placebo-controlled trials of ferroquine - a candidate anti-malarial drug - in adults with asymptomatic Plasmodium falciparum infection

(2011) Ghyslain Mombo-Ngoma et al.   MALARIA JOURNAL

A 2020 vision for vaccines against HIV, tuberculosis and malaria

(2011) Rino Rappuoli et al.   NATURE

Pharmacogenetics, Pharmacogenomics, and Individualized Medicine

(2011) Q. Ma et al.   PHARMACOLOGICAL REVIEWS

Artesunate Dose Escalation for the Treatment of Uncomplicated Malaria in a Region of Reported Artemisinin Resistance: A Randomized Clinical Trial

(2011) Delia Bethell et al.   PLoS One

A Pilot Randomised Trial of Induced Blood-Stage Plasmodium falciparum Infections in Healthy Volunteers for Testing Efficacy of New Antimalarial Drugs

(2011) James S. McCarthy et al.   PLoS One

Imaging of Plasmodium Liver Stages to Drive Next-Generation Antimalarial Drug Discovery

(2011) S. Meister et al.   SCIENCE

Live Attenuated Malaria Vaccine Designed to Protect Through Hepatic CD8+ T Cell Immunity

(2011) J. E. Epstein et al.   SCIENCE

Second generation analogues of RKA182: synthetic tetraoxanes with outstanding in vitro and in vivo antimalarial activities

(2011) Francesc Marti et al.   MedChemComm

A Research Agenda to Underpin Malaria Eradication

(2011) Pedro L. Alonso et al.   PLOS MEDICINE

A Randomized, Double-Blind, Placebo-Controlled Study to Investigate the Safety, Tolerability, and Pharmacokinetics of Single Enantiomer (+)-Mefloquine Compared with Racemic Mefloquine in Healthy Persons

(2010) Robert Tansley et al.   AMERICAN JOURNAL OF TROPICAL MEDICINE AND HYGIENE

Identification of a 1,2,4,5-Tetraoxane Antimalarial Drug-Development Candidate (RKA 182) with Superior Properties to the Semisynthetic Artemisinins

(2010) Paul M. O'Neill et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Synthesis and structure–activity relationships of novel benzoxaboroles as a new class of antimalarial agents

(2010) Yong-Kang Zhang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Drug- and non-drug-associated QT interval prolongation

(2010) Charlotte Van Noord et al.   BRITISH JOURNAL OF CLINICAL PHARMACOLOGY

Spirotetrahydro β-Carbolines (Spiroindolones): A New Class of Potent and Orally Efficacious Compounds for the Treatment of Malaria

(2010) Bryan K. S. Yeung et al.   JOURNAL OF MEDICINAL CHEMISTRY

Artesunate versus quinine in the treatment of severe falciparum malaria in African children (AQUAMAT): an open-label, randomised trial

(2010) Arjen M Dondorp et al.   LANCET

Thousands of chemical starting points for antimalarial lead identification

(2010) Francisco-Javier Gamo et al.   NATURE

Chemical genetics of Plasmodium falciparum

(2010) W. Armand Guiguemde et al.   NATURE

Erratum: Artemisinin resistance: current status and scenarios for containment

(2010) Arjen M. Dondorp et al.   NATURE REVIEWS MICROBIOLOGY

Rhinovirus Genome Evolution during Experimental Human Infection

(2010) Samuel Cordey et al.   PLoS One

Is the Tide Turning for New Malaria Medicines?

(2010) T. N. C. Wells   SCIENCE

Spiroindolones, a Potent Compound Class for the Treatment of Malaria

(2010) M. Rottmann et al.   SCIENCE

Discovery of Potent and Selective Inhibitors of CDPK1 from C. parvum and T. gondii

(2010) Ryan C. Murphy et al.   ACS Medicinal Chemistry Letters

Origin and Evolution of Sulfadoxine Resistant Plasmodium falciparum

(2010) Sumiti Vinayak et al.   PLoS Pathogens

Acquired Immunity to Malaria

(2009) D. L. Doolan et al.   CLINICAL MICROBIOLOGY REVIEWS

Structural Plasticity of Malaria Dihydroorotate Dehydrogenase Allows Selective Binding of Diverse Chemical Scaffolds

(2009) Xiaoyi Deng et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

New medicines to improve control and contribute to the eradication of malaria

(2009) Timothy N. C. Wells et al.   NATURE REVIEWS DRUG DISCOVERY

Artemisinin Resistance inPlasmodium falciparumMalaria

(2009) Arjen M. Dondorp et al.   NEW ENGLAND JOURNAL OF MEDICINE

High Resistance of Plasmodium falciparum to Sulphadoxine/Pyrimethamine in Northern Tanzania and the Emergence of dhps Resistance Mutation at Codon 581

(2009) Samwel Gesase et al.   PLoS One

African Genetic Diversity: Implications for Human Demographic History, Modern Human Origins, and Complex Disease Mapping

(2008) Michael C. Campbell et al.   Annual Review of Genomics and Human Genetics

The Antimalarial Trioxaquine DU1301 Alkylates Heme in Malaria-Infected Mice

(2008) F. Bousejra-El Garah et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

First Assessment in Humans of the Safety, Tolerability, Pharmacokinetics, and Ex Vivo Pharmacodynamic Antimalarial Activity of the New Artemisinin Derivative Artemisone

(2008) J. Nagelschmitz et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Antiparasitic Activities and Toxicities of Individual Enantiomers of the 8-Aminoquinoline 8-[(4-Amino-1-Methylbutyl)Amino]-6-Methoxy-4-Methyl-5-[3,4-Dichlorophenoxy]Quinoline Succinate

(2008) N. P. D. Nanayakkara et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Investigation of the Redox Behavior of Ferroquine, a New Antimalarial

(2008) Natascha Chavain et al.   MOLECULAR PHARMACEUTICS

Evidence of Artemisinin-Resistant Malaria in Western Cambodia

(2008) Harald Noedl et al.   NEW ENGLAND JOURNAL OF MEDICINE

Antigenic Variation in Trypanosoma brucei: Joining the DOTs

(2008) Chris Stockdale et al.   PLOS BIOLOGY