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KAF-156

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I UPAC name: 2-Amino-1-(2-(4-fluorophenyl)-3-((4-fluorophenyl)amino)-5,6-dihydro-8,8-dimethylimidazo(1,2-a)pyrazin-7(8H)-yl)ethanone   Molecular formula: C22H23F2N5O Molecular weight: 411.4 g/mol Synonyms: Ganaplacide, KAF-156, GNF-156, GNF 156 SMILES: CC1(C2=NC(=C(N2CCN1C(=O)CN)NC3=CC=C(C=C3)F)C4=CC=C(C=C4)F)C Developmental Status: Phase IIb combination study ongoing Company: Discovery partnership between MMV, Wellcome Trust, Novartis, and the Swiss Tropical and Public Health Institute Description: The imidazolopiperazine compound KAF156 belongs to a new class of antimalarial agents with activity against asexual and sexual blood stages and the pre-erythrocytic liver stages of malarial parasites. According to studies, KAF156 displayed activity against vivax and falciparum malaria, including artemisinin-resistant parasites. (White, N.J. et al., 2016). Mechanism of action: The mechanism of action of KAF156 could not yet be determined. Decreased susceptibility to KAF156...

ATOVAQUONE

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  Name: Atovaquone Synonym: Mepron, Wellvone, Acuvel Chemical formula: C 22 H 19 ClO 3 Molecular weight: 366.8 g/mol IUPAC name: 2-hydroxy-3-[(1r,4r)-4-(4-chlorophenyl)cyclohexyl]-1,4-dihydronaphthalene-1,4-dione SMILES: OC1=C([C@H]2CC[C@@H](CC2)C2=CC=C(Cl)C=C2)C(=O)C2=CC=CC=C2C1=O Indication:   It has antiprotozoal, antimicrobial and antipneumocystis activity and thus used for the treatment or prevention of Pneumocystis carinii pneumonia in patients who are intolerant to trimethoprim-sulfamethoxazole. Developmental stage: In combination with proguanil, it is available commercially as Malarone and used for the prevention and treatment of malaria caused by Plasmodium falciparum . Company: GlaxoSmithKline Description: Atovaquone or 2-(trans-4-(p-chlorophenyl)cyclohexyl)-3-hydroxy-1,4-naphthoquinone, is a hydroxynaphthoquinone analog of ubiquinone and an inhibitor of cytochrome bc 1 complex ( Mather et al., 2005) . It is found to be well tolerated, metab...

TAFENOQUINE

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Name: Tafenoquine Synonym: Etaquine, Krintafel, Arakoda, WR238605 Chemical formula: C 24 H 28 F 3 N 3 O 3 Molecular weight: 463.501 IUPAC name: N4-{2,6-dimethoxy-4-methyl-5-[3-(trifluoromethyl)phenoxy]quinolin-8-yl}pentane-1,4-diamine SMILES: COC1=CC(C)=C2C(OC3=CC=CC(=C3)C(F)(F)F)=C(OC)C=C(NC(C)CCCN)C2=N1 Indication: Tafenoquine is used for the treatment and prevention of relapsed infection caused by Plasmodium vivax in patients of age 16 years and above. Developmental stage: Phase III studies, developing as a single-dose treatment. Approved by US FDA July 2018 and by Australian TGA September 2018. Approved in first malaria-endemic country (Brazil) in October 2019 and in Thailand in December 2019 Under review in 5 endemic countries (MMV, Medicines for malaria venture). Company: GlaxoSmithKline; MMV About Plasmodium vivax malaria: Malaria caused by P. vivax have a significant impact on the health and economy of the population of South-Asia, South-East ...
Clinical trials to findout what can work against coronavirus (part 1) According to an article published in The Times of India, dated March 30 th , 2020, BCG or the bacillus Calmette-Guerin vaccine that has been used for ages to immunize new-borns to protect against tuberculosis, is being given to health-care workers in Melbourne to see if it can protect them against the deadly coronavirus. BCG, in addition to prevention against tuberculosis, has off-target benefits as well. It is a common immunotherapy for early-stage bladder cancer; it also seems to boost body’s immune system to fight infections better. The study reported is led by Nigel Curtis, at Murdoch Children’s Research Institute in Melbourne. According to him, BCG vaccine can boost the immune system and defend better against a range of viruses and bacteria. 4000 health care workers have volunteered to participate in a six-month trial to be vaccinated against seasonal influenza and TB, or the flu shot only. A placebo ...
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Erdafitinib Erdafitinib (also known as JNJ-42756493) is an orally bioavailable, pan fibroblast growth factor receptor (FGFR) inhibitor with potential antineoplastic activity. Upon oral administration, Erdafitinib binds to and inhibits FGFR, which may result in the inhibition of FGFR-related signal transduction pathways and thus the inhibition of tumour cell proliferation and tumour cell death in FGFR-overexpressing tumour cells. FGFR, upregulated in many tumour cell types, is a receptor tyrosine kinase essential to tumour cell proliferation, differentiation and survival. Astex Pharmaceuticals discovered this drug and licensed it to Janssen Pharmaceuticals for further development. Erdafitinib has been used in trials studying the basic science and treatment of Tumour or Lymphoma . Common Name:   Erdafitinib Synonyms :    JNJ-42756493; JNJ42756493; JNJ 42756493; G-024; JNJ-493 IUPAC Name :   N...
Drugs in Clinical Pipeline: Vatalanib Vatalanib [ N-(4-chlorophenyl)-4-(pyridine-4-ylmethyl)phthalazin-1-amine ] is an orally bioavailable anilinophthalazine compound that has potent antineoplastic activity. Vatalanib binds to and inhibits the protein kinase domain of vascular endothelial growth factor receptors 1 and 2 (VEGFR 1 and VEGFR2); both receptor tyrosine kinases are involved in angiogenesis. This agent also binds to and inhibits related receptor tyrosine kinases, including platelet-derived growth factor (PDGF) receptor, c-Kit, and c-Fms [1]. Preclinical studies demonstrated antitumor activity against a broad range of cancer types, including colorectal, prostate, renal, hepatocellular, myeloma, recurrent glioblastoma multiform and ovarian. The compound has been investigated in phase I/II studies, alone and in combination with chemotherapy. The activity of Vatalanib is as follows: IC 50  (VEGFR2/KDR, cell-free assay) = 37 nM IC 50  (VEGFR1/F...