ATP2A1 inhibitors(Sarcoplasmic/endoplasmic reticulum calcium ATPase 1 inhibitors), DHFR inhibitors(Dihydrofolate reductase inhibitors), DHPS inhibitors(Dihydropteroate synthase inhibitors)

+ [1]

Therapeutic Areas

Infectious Diseases

Active Indication

Malaria

Inactive Indication

Malaria, FalciparumSchistosomiasis Haematobia

Originator Organization

Dafra Pharma NV

Active Organization

Dafra Pharma NV

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date-

Regulation-

Structure/Sequence

Molecular FormulaC12H13ClN4

InChIKeyWKSAUQYGYAYLPV-UHFFFAOYSA-N

CAS Registry58-14-0

View All Structures (2)

Clinical Trials associated with Artesunate/Pyrimethamine/Sulfalene

NCT00510159

/ CompletedPhase 2/3

Randomized Double Blind Clinical Trial in Mali, Comparing the Effectiveness of Artesunate + Sulfamethoxypyrazine/Pyrimethamine Versus Praziquantel in the Treatment of S. Haematobium in Children

The purpose of this study is to evaluate the efficacy of praziquantel versus As+SMP (Co-Arinate FDC ®) in the treatment of Schistosoma haematobium in 6-15 year old Malian children. The nul-hypothesis in this study is that the combination of As+SMP is more effective than praziquantel in the treatment of S. haematobium infected children.

Start Date01 Aug 2007

Sponsor / Collaborator

Dafra Pharma NV

NCT00484900

/ CompletedPhase 3

Open Randomized Multi-Centre Trial, Comparing Artesunate-Sulfamethoxypyrazine-Pyrimethamine FDC Over 3 Days, Artesunate-Sulfamethoxypyrazine-Pyrimethamine FDC Over 48 Hours and Artemether-Lumefantrine FDC Over 3 Days on P. Falciparum Malaria

The purpose of this open randomised multi-centre clinical trial is to test the hypothesis that three pills of the fixed dose combination artesunate/sulfamethoxypyrazine/pyrimethamine, administered over 24 hours is not inferior in efficacy to the same drug administered over 48 hours and that the fixed dose combination artesunate/sulfamethoxypyrazine/pyrimethamine As/SMP fdc, independently of the duration of its dose interval, is not inferior in efficacy to 6 - 24 pills (number of pills administered to respectively children and adults)of the 60 hours treatment of artemether/lumefantrine for the treatment of uncomplicated P. falciparum malaria.

Start Date01 May 2006

Sponsor / Collaborator

Dafra Pharma NV

NCT00127998

/ CompletedNot ApplicableIIT

Characterization of Novel Molecular Tools for the Epidemiological Surveillance of Antimalarial Drug Resistance in Mali

Resistance of Plasmodium falciparum (malaria) to current antimalarial drugs and the continuing development of resistance to new antimalarial formulations is one of the major obstacles to effective malaria control and case management. Efficient, comprehensive and validated methods for monitoring drug resistance in advance of the development of resistance to the antimalarial drugs that are in use are urgently needed. Molecular markers of genetic polymorphisms that give rise to resistant P. falciparum parasites and methods in population genetics for evaluating the data can be valuable tools for monitoring drug resistance in the field. This study aims to:
Prospectively measure the in vivo response of P. falciparum malaria in Mali to several different antimalarial drugs and drug combinations: chloroquine (CQ), sulfadoxine-pyrimethamine (SP), amodiaquine (AQ), sulfadoxine-pyrimethamine in combination with amodiaquine (SP/AQ), amodiaquine in combination with artesunate (AQ/AS), sulfadoxine-pyrimethamine in combination with artesunate (SP/AS), and artemether-lumefantrine (Co-artem). In one site with preliminary data showing a high rate of P. falciparum resistance to mefloquine (MQ), this drug will also be tested.
Measure the frequencies of molecular markers for antimalarial drug resistance, and examine how those results relate to the efficacy of these drugs in treating clinical malaria
Measure drug levels at 3 days and correlate with efficacy results.
Examine early clinical, parasitologic, and clinical predictors of late treatment failure.
Use the knowledge gained in Aims 1-3 to develop a molecular tool for a countrywide resistance surveillance system for antimalarial drugs.

Start Date01 Jul 2005

Sponsor / Collaborator

Centers for Disease Control & Prevention

100 Clinical Results associated with Artesunate/Pyrimethamine/Sulfalene

100 Translational Medicine associated with Artesunate/Pyrimethamine/Sulfalene

100 Patents (Medical) associated with Artesunate/Pyrimethamine/Sulfalene

Literatures (Medical) associated with Artesunate/Pyrimethamine/Sulfalene

01 Sep 2018·Infection, Genetics and EvolutionQ3 · MEDICINE

Spatio-temporal distribution of PfMDR1 polymorphism among uncomplicated Plasmodium falciparum malaria cases along international border of north east India

Q3 · MEDICINE

Article

Author: Goomber, Shelly ; Anvikar, Anup ; Valecha, Neena ; Mishra, Neelima ; Yadav, Chander Prakash

PfMDR1 single nucleotide polymorphisms (SNP) are good correlate markers for antimalarial drug resistance worldwide. Present study is a comprehensive view of screening of PfMDR1 polymorphism to antimalarials practiced with geography and time. Study sites Mizoram, Tripura, Meghalaya chosen are at multivariate drug pressure due to cross border migration and transmission. Mizoram is gateway to south east Asia through Myanmar whereas Tripura, Meghalaya share porous border with Bangladesh. Baseline finger pricked blood stained filter paper for confirmed uncomplicated Plasmodium falciparum infected patients (year 2015) were obtained from National Institute of Malaria Research, New Delhi, India. PfMDR1 polymorphism for codon N86Y, Y184F, D1246Y was determined by PCR-RFLP, further confirmed by sequencing. There observed marked predominance of Plasmodium isolates with PfMDR1 wild type alleles for all codons under study i.e. 86, 184, 1246. Spatially, Plasmodium isolates from Mizoram were most diverse with co-existence of PfMDR1 genotype with NYD, YYD, NFD haplotypes, followed by Tripura. Isolates from Meghalaya were of all NYD haplotype. Reports, referring to screening of PfMDR1 SNPs to CQ/SP/AS-SP across India, were archived. Temporal study show distinct rise in proportion of PfMDR1 wild type N86 allele since introduction of Artemether-Lumefantrine as first line antimalarial. Hence spatio-temporal screening of Plasmodium population with PfMDR1 single nucleotide polymorphism accounts for its association with antimalarial susceptibility and validate PfMDR1 SNPs as antimalarial drug resistant marker.

01 Apr 2015·Infection, Genetics and EvolutionQ3 · MEDICINE

High prevalence of pfdhfr–pfdhps triple mutations associated with anti-malarial drugs resistance in Plasmodium falciparum isolates seven years after the adoption of sulfadoxine–pyrimethamine in combination with artesunate as first-line treatment in Iran

Q3 · MEDICINE

Article

Author: Rouhani, Maryam ; Djadid, Navid Dinparast ; Pirahmadi, Sakineh ; Zakeri, Sedigheh ; Raeisi, Ahmad

The spread of anti-malarial drug resistance will challenge any malaria control and elimination strategies, and routine monitoring of resistance-associated molecular markers of commonly used anti-malarial drugs is very important. Therefore, in the present investigation, the extent of mutations/haplotypes in dhfr and dhps genes of Plasmodium falciparum isolates (n=72) was analyzed seven years after the introduction of sulfadoxine-pyrimethamine (SP) plus artesunate (AS) as first-line anti-malarial treatment in Iran using PCR-RFLP methods. The results showed that the majority of the patients (97.2%) carried both 59R and 108N mutations in pure form with wild-type genotype at positions N51 and I164. Additionally, a significant increase (P<0.05) was observed in the frequency of R59N108/G437 haplotype (79.2%) during 2012-2014. This raise was because of the significant increase (P<0.05) in the frequency of 437G mutation (81.9%), which more likely was due to more availability of SP as anti-malarial drug for treatment of falciparum patients in these malaria-endemic areas of Iran. However, no quintuple mutations associated with treatment failure were detected. In conclusion, the present results along with in vivo assays suggest that seven years after the adoption of SP-AS as the first-line treatment in Iran, this drug remains efficacious for treatment of uncomplicated falciparum malaria, as a partner drug with AS in these malaria-endemic areas.

01 May 2012·Antimicrobial Agents and ChemotherapyQ2 · MEDICINE

Comparative Efficacies of Artemisinin Combination Therapies in Plasmodium falciparum Malaria and Polymorphism of pfATPase6 , pfcrt , pfdhfr , and pfdhps Genes in Tea Gardens of Jalpaiguri District, India

Q2 · MEDICINE

Article

Author: Biswas, Asit ; Maji, Ardhendu K. ; Bera, Dilip K. ; Ray, Krishnangshu ; Mullick, Shrabanee ; Guha, Subhasish K. ; Saha, Pabitra ; Kundu, Pratip K. ; Das, Sonali ; Das, Madhusudan ; Chattopadhyay, Gaurangadeb ; Ganguly, Swagata

ABSTRACT In India, chloroquine has been replaced by a combination of artesunate and sulfadoxine-pyrimethamine (AS-SP) for uncomplicated P. falciparum malaria. Other available combinations, artemether-lumefantrine (AM-LF) and artesunate-mefloquine (AS-MQ), not included in the national program, are widely used by private practitioners. Little is known about the therapeutic efficacy of these artemisinin combinations and the prevalence of molecular markers associated with antimalarial drug resistance. A total of 157 patients with P. falciparum monoinfection were recruited and randomized into three study groups (AS-SP, AM-LF, and AS-MQ). All patients were followed up for 42 days to study the clinical and parasitological responses according to the WHO protocol (2009). We assessed the polymorphism of the pfATPase6 , pfcrt , pfdhfr , and pfdhps genes by the DNA-sequencing method. The PCR-corrected therapeutic efficacies of AS-SP, AM-LF, and AS-MQ were 90.6% (95% confidence interval [CI], 0.793 to 0.969), 95.9% (95% CI, 0.860 to 0.995), and 100% (95% CI, 0.927 to 1.00), respectively. No specific mutational pattern was observed in the pfATPase6 gene. All isolates had a K76T mutation in the pfcrt gene. In the pfdhfr-pfdhps genotype, quadruple mutation was frequent, and quintuple mutation was documented in 6.3% of P. falciparum isolates. The significant failure rate of AS-SP (9.5%), although within the limit (10%) for drug policy change, was due to SP failure because of prevailing mutations in pfdhfr , I 51 R 59 N 108 , with pfdhps , G 437 and/or E 540 . The efficacy of this ACT needs periodic monitoring. Artemether-lumefantrine and artesunate-mefloquine are effective alternatives to the artesunate-sulfadoxine-pyrimethamine combination.

100 Deals associated with Artesunate/Pyrimethamine/Sulfalene

External Link

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R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Malaria	-	Dafra Pharma NV	-

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Schistosomiasis Haematobia	Discovery	Mali	Dafra Pharma NV	01 Aug 2007
Malaria, Falciparum	Discovery	Rwanda	Dafra Pharma NV	01 May 2006
Malaria, Falciparum	Discovery	Cameroon	Dafra Pharma NV	01 May 2006
Malaria, Falciparum	Discovery	Mali	Dafra Pharma NV	01 May 2006
Malaria, Falciparum	Discovery	Sudan	Dafra Pharma NV	01 May 2006

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