Page last updated: 2024-12-05

lucanthone hydrochloride

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Description

Lucanthone hydrochloride is a synthetic antiparasitic drug that was originally developed in the 1940s to treat schistosomiasis. It is a derivative of the dye Trypan Blue and was the first effective oral treatment for the disease. It works by inhibiting the enzyme glutathione reductase, which is essential for the survival of Schistosoma parasites. However, it is no longer commonly used due to its significant side effects, including hepatotoxicity and neurotoxicity. Despite its limited clinical use, lucanthone hydrochloride continues to be studied as a potential lead compound for the development of new antiparasitic drugs. Researchers are investigating its mechanism of action and exploring its potential to be used in combination therapy with other drugs.'

Schistosomicides: Agents that act systemically to kill adult schistosomes. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID11054
CHEMBL ID2007389
SCHEMBL ID419165
MeSH IDM0012718

Synonyms (64)

Synonym
3735 r.p.
lucanthone hydrochloride [usan:usp]
unii-918k9n56qz
1-diaethylamino-aethylamino-4-methyl-thioxanthonhydrochlorid
lucanthone hcl
schistosomicides
918k9n56qz ,
79 t61
b.w. 57-233
scapuren
3735 r. p.
lucanthone monohydrochloride
schistosomicide
1-(.beta.-diethylaminoethylamino)-4-methyl-thiaxanthone hydrochloride
ms. 752
nilodin
tixantone
nih 3127
wln: t c666 bs ivj d1 gm2n2&2 &gh
miracol
nsc-14574
nsc 14574
1-[[2-(diethylamino)ethyl]amino]-4-methylthioxanthen-9-one monohydrochloride
miracil d
1-[[2-(diethylamino)ethyl]amino]-4-methylthiaxanthone hydrochloride
miracil d hydrochloride
79t61
bw 57223
cbc 900139
548-57-2
dr-15771
lucanthone hydrochloride
lucanthone hydrochloride (usan)
D04791
9h-thioxanthen-9-one, 1-((2-(diethylamino)ethyl)amino)-4-methyl-, monohydrochloride
bw 57-233
1-(beta-diethylaminoethylamino)-4-methylthiaxanthone hydrochloride
lucanthone hydrochloride [usan]
einecs 208-951-5
thioxanthen-9-one, 1-(2-(diethylaminoethyl)amino)-4-methyl-, monohydrochloride
ai3-52847
1-diaethylamino-aethylamino-4-methyl-thioxanthonhydrochlorid [german]
1-((2-(diethylamino)ethyl)amino)-4-methylthioxanthen-9-one monohydrochloride
1-((2-diethylaminoethyl)amino)-4-methylthioxanthen-9-one hydrochloride
hsdb 7095
1-(2-diethylaminoethylamino)-4-methylthiaxanthone hydrochloride
1-[[2-(diethylamino)ethyl]amino]-4-methyl-9h-thioxanthen-9-one hydrochloride
79-t61
CHEMBL2007389
rp-3735
ms-752
FT-0670871
SCHEMBL419165
1-((2-(diethylamino)ethyl)amino)-4-methyl-9h-thioxanthen-9-one hydrochloride
lucanthone hydrochloride [hsdb]
lucanthone hydrochloride [mi]
Q27271388
lucanthone hydrochloride 100 microg/ml in acetonitrile
DTXSID20878506
1-[2-(diethylamino)ethylamino]-4-methylthioxanthen-9-one;hydrochloride
CS-0109668
lucanthone (hydrochloride)
HY-B2098A
AKOS040758605

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" A linear relationship was established between the LD50 values of hycanthone analogs in mice and 1) the Ki values obtained from the inhibition of [3H]quinuclidinyl benzilate binding to the muscarinic receptors of N4TG1 neuroblastoma cells; 2) the I50 values obtained from the inhibition of alpha-amylase secretion induced by carbachol in pancreatic acini cells; and 3) the KB values obtained from the inhibition of guinea-pig ileum contraction induced by acetylcholine."( Antimuscarinic activities of hycanthone analogs: possible relationship with animal toxicity.
Chiang, PK; Gordon, RK, 1986
)
0.27
"The present study using a murine model heavily infected with Schistosoma japonicum aimed to elucidate the pathogenesis of adverse effects of praziquantel treatment of schistosome-infected subjects."( Adverse effects of praziquantel treatment of Schistosoma japonicum infection: involvement of host anaphylactic reactions induced by parasite antigen release.
Matsumoto, J, 2002
)
0.31
"87 microg/ml, respectively, but no toxic effects of other drugs on schistosome worms were found."( [Toxicity of several drugs against Schistosoma japonicum adult worms in vitro].
Hua, WQ; Qian, CY; Song, LJ; Wang, J; Xu, YL; Yin, XR; Yu, CX; Zeng, HH; Zhang, W, 2011
)
0.37

Pharmacokinetics

ExcerptReferenceRelevance
" The pharmacokinetic parameters (mean +/- SD) in the rabbit and rat, respectively, were as follows: plasma clearance, 65."( Pharmacokinetics of oxamniquine in rabbit and rat.
Indalo, AA; Kokwaro, GO; Taylor, G,
)
0.13
" Hence, it would be expected that in PCM rats, some pharmacokinetic parameters of oltipraz are fully or partially returned to controls by cysteine."( Effects of cysteine on the pharmacokinetics of oltipraz in rats with protein-calorie malnutrition.
Bae, SK; Kim, JW; Kim, T; Kwon, JW; Lee, MG; Yang, SH, 2005
)
0.33
"Oltipraz was given intravenously (10 mg x kg(-1)) or orally (30 mg x kg(-1)) to rats with liver cirrhosis induced by N-dimethylnitrosamine (LC rats) or with diabetes, induced by streptozotocin (DM rats) or to rats with both liver cirrhosis and diabetes (LCD rats) and to control rats, and pharmacokinetic variables measured."( Pharmacokinetics of oltipraz in diabetic rats with liver cirrhosis.
Ahn, CY; Bae, SH; Bae, SK; Jung, YS; Kim, T; Kim, YC; Lee, MG; Shin, WG, 2009
)
0.35
" mansoni worms together with a biological, pharmacokinetic and toxicological in silico evaluation."( Antiparasitic, structural, pharmacokinetic, and toxicological properties of riparin derivatives.
Batista, LF; da Silva Filho, AA; de Moraes, J; de Oliveira, MAR; Gutierrez, SJC; Lago, EM; Mafud, AC; Mascarenhas, YP; Mengarda, AC; Nunes, GBL; Pinto, PLS; Rubio, TI; Silva, MPN; Xavier, RP, 2018
)
0.48
" mansoni, as well as the in silico determination of pharmacokinetic parameters for the prediction of the oral bioavailability of these derivatives."( In vitro activity, ultrastructural studies and in silico pharmacokinetic properties of indol-3-yl-thiosemicarbazones derivatives and analogues against juvenile and adult worms of S. mansoni.
Alves, LC; Brayner, FA; da Rocha, RET; da Silva, AL; da Silva, RMF; de Almeida Júnior, ASA; de Azevedo Albuquerque, MCP; de Oliveira, JF; do Carmo Alves de Lima, M; Gouveia, ALA; Junior, NCP, 2019
)
0.51
" Pharmacokinetic parameters were measured in naive mice."( Efficacy, metabolism and pharmacokinetics of Ro 15-5458, a forgotten schistosomicidal 9-acridanone hydrazone.
Caffrey, CR; Charman, SA; Dong, Y; El-Sakkary, N; Gangoiti, J; Häberli, C; Huang, J; Keiser, J; Momper, JD; Probst, A; Siegel, D; Skinner, DE; Ta, AP; Vennerstrom, JL; Vigneron, S, 2020
)
0.56
"The present work aimed to carry out in vitro biological assays of thiazole compounds against adult worms of Schistosoma mansoni, as well as the in silico determination of pharmacokinetic parameters to predict the oral bioavailability of these compounds."( In vitro activity, ultrastructural analysis and in silico pharmacokinetic properties (ADMET) of thiazole compounds against adult worms of Schistosoma mansoni.
Aires, AL; Albuquerque, MCPA; Alves, LC; Araújo, HDA; Brayner, FA; Cruz Filho, IJD; Lima, MDCA; Marques, DSC; Nascimento, PHDB; Rocha, JVRD; Silva, DVSPD, 2023
)
0.91

Compound-Compound Interactions

ExcerptReferenceRelevance
"The purpose of the study is to explore the efficacy of mefloquine administered orally at single, multiple doses, or in combination with artesuante, artemether, or praziquantel in mouse--Schistosoma japonicum model."( Effect of mefloquine administered orally at single, multiple, or combined with artemether, artesunate, or praziquantel in treatment of mice infected with Schistosoma japonicum.
Jiao, PY; Mei, JY; Xiao, SH, 2011
)
0.37
" The results highlighted the possibility of using (ω-3) PUFA combined with ART as a novel anti-schistosomal combination therapy."( Effect of omega-3 fatty acids administered as monotherapy or combined with artemether on experimental Schistosoma mansoni infection.
Abd El-Mageed, SA; Abdalla, HA; El-Beshbishi, SN; El-Nemr, HEE; Saleh, NE; Shebl, AM; Taman, A, 2019
)
0.51
"This study aimed to evaluate the efficacy of gamma-aminobutyric acid (GABA) alone or combined with praziquantel (PZQ) against Schistosoma (S) mansoni infection in a murine model."( Schistosomicidal and hepatoprotective activity of gamma-aminobutyric acid (GABA) alone or combined with praziquantel against Schistosoma mansoni infection in murine model.
Fahmy, AM; Hegab, A; Tm, D; William, S, 2022
)
0.72
" Significant improvement in hepatic oxidative stress levels, serum albumin and total protein in response to GABA treatment alone or combined with PZQ."( Schistosomicidal and hepatoprotective activity of gamma-aminobutyric acid (GABA) alone or combined with praziquantel against Schistosoma mansoni infection in murine model.
Fahmy, AM; Hegab, A; Tm, D; William, S, 2022
)
0.72

Bioavailability

ExcerptReferenceRelevance
"The bioavailability of the new antischistosomal agent, oltipraz, was examined under three different dietary conditions in seven healthy males."( Diet-controlled blood levels of oltipraz in healthy male subjects.
Ali, HM; Bennett, JL; Homeida, MM; Sulaiman, SM, 1984
)
0.27
" When 6 healthy adult animals were given oltipraz together with cysteine in a crossover study, peak serum concentrations, areas under the curve and absorption rate constants of oltipraz were on average 7 times greater than when the drug was administered alone."( Effect of cysteine on oltipraz blood levels in green monkeys (Cercopithecus aethiops).
Ali, HM; Bennett, JL; Homeida, MM; Sulaiman, SM, 1984
)
0.27
" This effect may be due to the low bioavailability of PZQ that has a low hydrosolubility and fast metabolism."( Improvement of antischistosomal activity of praziquantel by incorporation into phosphatidylcholine-containing liposomes.
Costa, PI; Gremião, MP; Mourão, SC; Salgado, HR, 2005
)
0.33
" There was no marked difference of the absorption rate between rats with and without ligated bile duct in rat intestinal permeability technique."( [Optimization and evaluation of a new antischistosomal drug QH917 self-microemulsifying drug delivery system].
Gan, L; Gan, Y; Pan, WS; Zhang, JY; Zhu, CL, 2007
)
0.34
"Solid dispersions have been used as a strategy to improve the solubility, dissolution rate, and bioavailability of poor water-soluble drugs."( Solid dispersions of imidazolidinedione by PEG and PVP polymers with potential antischistosomal activities.
de Lima, Mdo C; de Oliveira, BG; De Simone, CA; Galdino, SL; Guedes, FL; Hernandes, MZ; Neto, PJ; Pitta, IR; Veiga, FJ, 2011
)
0.37
" Despite ex vivo activity, none of the compounds tested was active in vivo, suggesting that the limited bioavailability may compromise compound activity."( Synthesis and evaluation of 1,4-naphthoquinone ether derivatives as SmTGR inhibitors and new anti-schistosomal drugs.
Becker, K; Belorgey, D; Chessé, M; Davioud-Charvet, E; Day, L; Huang, HH; Johann, L; Williams, DL, 2015
)
0.42
"Our study identified schistosocidal leads with high bioavailability profile and the exploration of binding modes could lay the foundation for synthetic modification of the plant metabolites for the development of novel anti-schistosoma drug(s) with new mechanism of action."( Structure-Based Study of Natural Products with Anti-Schistosoma Activity.
Akachukwu, I; John, MC; Justina, NN; Kosisochukwu, A; Olubiyi, OO, 2017
)
0.46
" The treatment of choice presents low bioavailability and water solubility, in addition to the induction of parasite resistance."( Nanotechnology as a potential therapeutic alternative for schistosomiasis.
Assolini, JP; Bortoleti, BTDS; Chagas, AF; Conchon-Costa, I; Costa, IN; Machado, LF; Melanda, FN; Miranda-Sapla, MM; Oliveira, FJA; Pavanelli, WR; Sahd, CS; Tomiotto-Pellissier, F, 2017
)
0.46
" Unfortunately, it exhibits low oral bioavailability which can compromise its efficacy."( Niosomes for enhanced activity of praziquantel against Schistosoma mansoni: in vivo and in vitro evaluation.
Abd Elazeem, MA; Aboul Asaad, IA; El Maghraby, GM; El-Kowrany, SI; El-Nouby, KA; Zoghroban, HS, 2019
)
0.51
" mansoni eggs hatchability and viability, a ground for its use in chemotherapy of schistosomiasis mansoni and japonicum because of its increased bioavailability in the gastrointestinal tract."( In vitro effect of curcumin on Schistosoma species viability, tegument ultrastructure and egg hatchability.
Abou El Dahab, MM; Mahana, NA; Mahmoud, SSM; Shahat, SM, 2019
)
0.51
" This work aimed to improve the therapeutic outcome of the only available antischistosomal drug worldwide, praziquantel (PZQ), by incorporating it into a novel carrier, "solid lipid nanoparticles (SLNs)", to enhance its solubility, bioavailability and efficacy."( A novel praziquantel solid lipid nanoparticle formulation shows enhanced bioavailability and antischistosomal efficacy against murine S. mansoni infection.
Al-Shorbagy, MY; Botros, S; El-Feky, GS; El-Lakkany, NM; Radwan, A; Saleh, S; William, S, 2019
)
0.51
"SLN-PZQ demonstrated enhanced PZQ bioavailability and antischistosomal efficacy with a safe profile despite the prolonged residence in the systemic circulation."( A novel praziquantel solid lipid nanoparticle formulation shows enhanced bioavailability and antischistosomal efficacy against murine S. mansoni infection.
Al-Shorbagy, MY; Botros, S; El-Feky, GS; El-Lakkany, NM; Radwan, A; Saleh, S; William, S, 2019
)
0.51
" mansoni, as well as the in silico determination of pharmacokinetic parameters for the prediction of the oral bioavailability of these derivatives."( In vitro activity, ultrastructural studies and in silico pharmacokinetic properties of indol-3-yl-thiosemicarbazones derivatives and analogues against juvenile and adult worms of S. mansoni.
Alves, LC; Brayner, FA; da Rocha, RET; da Silva, AL; da Silva, RMF; de Almeida Júnior, ASA; de Azevedo Albuquerque, MCP; de Oliveira, JF; do Carmo Alves de Lima, M; Gouveia, ALA; Junior, NCP, 2019
)
0.51
"The present work aimed to carry out in vitro biological assays of thiazole compounds against adult worms of Schistosoma mansoni, as well as the in silico determination of pharmacokinetic parameters to predict the oral bioavailability of these compounds."( In vitro activity, ultrastructural analysis and in silico pharmacokinetic properties (ADMET) of thiazole compounds against adult worms of Schistosoma mansoni.
Aires, AL; Albuquerque, MCPA; Alves, LC; Araújo, HDA; Brayner, FA; Cruz Filho, IJD; Lima, MDCA; Marques, DSC; Nascimento, PHDB; Rocha, JVRD; Silva, DVSPD, 2023
)
0.91

Dosage Studied

ExcerptRelevanceReference
" A dosage schedule of hycanthone which was too small to have any significant chemotherapeutic effect in mice (3 X 3 mg/kg) was sufficient to induce a statistically highly significant incidence of micronodular lesions and of precancerous nodules."( Long-term hepatocellular effects of hycanthone and of two other anti-Schistosomal drugs in mice infected with Schistosoma mansoni.
Bueding, E; Haese, WH, 1976
)
0.26
" in mice and hamsters was 50 mg/kg body weight after a single oral dose and 20 or 50 mg/kg body weight respectively when dosed once daily on 5 consecutive days."( [Experimental studies on the schistosomicidal activity of the aminobenzaldehyde derivative 80.647 (author's transl)].
Ascher, G; Hildebrandt, J; Mieth, H; Reinshagen, H, 1977
)
0.26
" When artemether was given ig or im to mice infected with Schistosoma japonicum for 32-35 d at the dosage of 1/10-1/2 LD50."( [Effect of artemether against Schistosoma japonicum].
Mei, JY; Xiao, SH; You, JQ, 1992
)
0.28
"The effect of Ro 15-5458 (10-2-(diethylamino)ethyl-9-acridanone(2-thiazolin- 2-yl)hydrazone) on the steady-state RNA levels of Schistosoma mansoni was studied after dosing the host with 15 mg kg-1 and retrieving parasites."( The schistosomicidal compound Ro 15-5458 causes a reduction in the RNA content of Schistosoma mansoni.
Bennett, JL; Eshete, F, 1991
)
0.28
" Control mice and mice infected with Schistosoma mansoni were dosed with PZQ and their urines were examined for the presence of metabolites using a triple-quadrupole mass spectrometer (tandem mass spectrometer)."( Metabolism studies of the antischistosomal drug praziquantel using tandem mass spectrometry: qualitative identification of 17 hydroxylated metabolites from mouse urine.
Abramson, FP; Ali, MH; Cohn, VH; Fetterolf, DD, 1990
)
0.28
" Oltipraz was found to be active in reducing the number of worms significantly only when administered in a higher dosage 2 hours before infection and 7 days after infection."( The prophylactic and curative effect of oltipraz in experimental schistosomiasis mansoni in mice.
Aboul-Atta, AM, 1990
)
0.28
"We evaluated a variety of biochemical parameters in Schistosoma mansoni isolated from mice up to 4 days after dosing with 15 mg/kg Ro 15-5458."( Schistosoma mansoni: biochemical characteristics of the antischistosomal effects of Ro 15-5458.
Bennett, JL; Eshete, F, 1990
)
0.28
"Mice infected with adult Schistosoma mansoni were dosed with a single oral dose of 125 or 250 mg/kg oltipraz, 50 or 100 mg/kg oxamniquine, or 200 or 400 mg/kg praziquantel."( Rate of action of schistosomicides in mice infected with Schistosoma mansoni.
Bruce, JI; Coles, GC; de Souza, CP; Dias, EP; Katz, N,
)
0.13
" Percent reduction in worm burden in mice treated with levo-PZQ was significantly higher than in those with PZQ at a dosage of 2 x 50 mg/kg (67."( A comparison of the antischistosomal effect of levo- and dextro-praziquantel on Schistosoma japonicum and S. mansoni in mice.
Irie, Y; Nara, T; Ohmae, H; Tanaka, M; Utsunomiya, H; Yasuraoka, K, 1989
)
0.28
"A field trial has been carried out in Sudan to determine the optimum dosage regimen for the use of Oltipraz in the treatment of Schistosoma mansoni in schoolchildren."( Dose-finding trial using Oltipraz to treat schoolchildren infected with Schistosoma mansoni in Gezira, Sudan.
Daffalla, AA; Dixon, HG; el Igail, AB; el Tayeb, M; Fenwick, A; Kardaman, MW, 1985
)
0.27
" A very low dosage of hycanthone (0."( Failure of targeted mass treatment to control schistosomiasis.
Manshande, JP; Polderman, AM, 1981
)
0.26
"The effects of Astiban, Lucanthone, Hycanthone and Niridazole on autophagic activities in the gastrodermis of Schistosoma mansoni were determined in vivo, using different dosage levels and dosage times."( Schistosoma mansoni: an in vivo study of drug-induced autophagy in the gastrodermis.
Clarkson, J; Erasmus, DA, 1984
)
0.27
" Thus, the same parasitological cure could be achieved by oltipraz as well as by praziquantel, but with a lower dosage of oltipraz."( Comparative trial of oltipraz versus praziquantel in the treatment of urinary schistosomiasis in the Gabon.
Baltes, R; Burchard, GD; Dietrich, M; Kern, P, 1984
)
0.27
" The results showed that administration of ambilhar to guinea pigs dosed with lead acetate resulted in a significant decrease in the liver content of lead with a concomitant increase in urinary and faecal lead excretion."( Some studies on the effects of ambilhar on mobilisation and excretion of lead.
Abdel Aziz, FT; Al-Khayat, TM, 1981
)
0.26
" Six weeks after dosing the treated rabbits and untreated controls were killed and examined."( Histological changes elicited in Schistosoma japonicum infected rabbits following curative chemotherapy with 4-isothiocyano-4'-nitro-diphenylamine (C9333-Go/CGP 4540).
Lewert, RM; Robinson, A, 1981
)
0.26
" Both compounds reach peak levels in blood within two hours after oral dosing and are detectable for at least eight hours."( Levels of metrifonate and dichlorvos in plasma and erythrocytes during treatment of schistosomiasis with Bilarcil.
Bengtsson, E; Holmstedt, B; Nordgren, I; Pettersson, BM, 1981
)
0.26
"After a brief reassessment of the pathogenic problem, the authors review the presently available drugs and their respective dosage and side-effects."( [Medical treatment of schistosomiasis (author's transl)].
Barabe, P; De Lajudie, JP; Perrot, JP,
)
0.13
"6% of the administered dosage and that in feces 24."( [Pharmacokinetics of artenibenzoate in rats].
Ji, XJ; Li, HY; Wu, LJ; Xu, PS; Zhang, FR, 1995
)
0.29
" In infected mice treated ig with Art at the same dosage for 24 h, the inhibition rates of alkaline phosphatase (AKP) activity in female and male worms were 30% and 25%, respectively."( [Effect of artemether on glycogen, protein, alkaline phosphatase and acid phosphatase of Schistosoma japonicum].
Feng, J; Guo, H; Jiao, P; Mei, J; Xiao, S; Yao, M; You, J, 1994
)
0.29
" In infected rabbits treated repeatedly with the above-mentioned dosage of Art at 2-wk intervals (i."( [Pathological changes in the livers of rabbits infected with schistosome cercariae and treated with artemether or praziquantel in the early stage of infection].
Xiao, S; Yang, Y; Zhang, C, 1995
)
0.29
"kg-1 and followed by the repeated dosing at 2-3 wk intervals, the total and female worm reduction rates as compared with the control were evident."( Effect of early treatment of artemether against schistosomiasis in mice.
Jiao, PY; Mei, JY; Xiao, SH; You, JQ, 1994
)
0.29
" When the drug was given at a daily dosage of 200 mg/kg for 4 successive days from 46 days post-infection, a significant reduction in worm recovery was observed."( Studies on chemotherapy of parasitic helminths: efficacy of artemether on Japanese strain of Schistosoma japonicum in mice.
Akyol, CV; Ishih, A; Ito, M; Sano, M; Tungtrongchitr, A, 1993
)
0.29
" In Art group, the first dose of 6 mg/kg was given in late August, followed by repeated dosing every 15 days for 3 times."( [Field studies on preventive effect of artemether against infection with Schistosoma japonicum].
Chen, M; Chu, B; Shi, Z; Wang, C; Xiao, S; Zhang, Z; Zheng, J; Zhuo, S, 1995
)
0.29
" When rabbits were treated ig with artemether 10 mg kg-1 on day 7 after infection, followed by repeated dosing every week for 4 times, some parameters related to acute schistosomiasis, such as temperature, eosinophil count and eggs in the feces were negative, and low specific antigen and antibody levels in serum were seen."( Experimental studies on early treatment of schistosomal infection with artemether.
Wang, CZ; Xiao, SH; Yang, YQ; You, JQ, 1995
)
0.29
" The results showed that in mice a promising effect was obtained when an initial dose of Art 300 mg/kg was given ig on d7 after infection with cercariae, followed by repeated dosing every wk for 4 times."( [Experimental studies on the preventive effect of artemether against schistosomal infection].
Guo, H; Jiao, P; Mei, J; Xiao, S; Yang, Y; You, J, 1995
)
0.29
" Induction of glutathione S-transferase, gamma-glutamylcysteine synthetase and DT-diaphorase has been observed in human tissues following the administration of a single oral dosage of oltipraz."( Chemopreventive activity of oltipraz.
Clapper, ML, 1998
)
0.3
"kg-1 on d 21 after infection, followed by the repeated dosing once every 1 or 2 wk for 2-4 times."( Microscopic observations on livers of rabbits and dogs infected with Schistosoma japonicum cercariae and early treatment with artemether or praziquantel.
Xiao, SH; Yang, YQ; You, JQ; Zhang, CW, 1996
)
0.29
" on d 7-15 after infection, followed by repeated dosing once every 7-15 d for a total of 3 doses."( Preventive effect of artemether in rabbits infected with Schistosoma japonicum cercariae.
Feng, Z; Guo, HF; Jiao, PY; Mei, JY; Xiao, SH; You, JQ, 1998
)
0.3
" Treatment with praziquantel at a dosage of 40 mg per kilogram of body weight was given in October 1991 and October 1992 to 460 individuals (group A)."( Evidence for a long-term effect of a single dose of praziquantel on Schistosoma mansoni-induced hepatosplenic lesions in northern Uganda.
Doehring, E; Frenzel, K; Grigull, L; Loroni-Lakwo, T; Ndugwa, CM; Odongo-Aginya, E; Schweigmann, U; Spannbrucker, N; Vester, U, 1999
)
0.3
"Data on age, height and mid upper-arm circumference (MUAC) from nearly 6000 schoolchildren in Ghana, Tanzania and Malawi (not MUAC) were used to examine their power to predict bodyweight and thus the dosage of praziquantel required to treat schistosomiasis."( Alternatives to bodyweight for estimating the dose of praziquantel needed to treat schistosomiasis.
Adjei, S; Bobrow, E; Bundy, D; de Graft-Johnson, J; Hall, A; Kihamia, C; Mwanri, L; Nokes, C; Wen, ST,
)
0.13
" This technique provided conditions for the separation of the active ingredient from the dosage form by extraction in methanol."( Determination of oxamniquine in capsules by HPLC.
Almeida, AE; Gremião, MP; Pierri, EG, 2001
)
0.31
"The RNA and DNA contents of female worms recovered from the host 48 h after dosing were markedly decreased by 51."( [Effect of artemether on nucleoside uptake and nucleic acid content in Schistosoma japonicum].
Mei, J; Xiao, S; Yao, M; You, J; Zhai, Z, 1999
)
0.3
" Group II received the same dosage of placebo at the corresponding times."( [Field application of oral artesunate for preventing Schistosoma japonicum infection].
Chen, J; Fang, G; Li, J; Li, S; Ou, N; Wang, Q; Wang, T; Xu, M; Zhang, S; Zhang, X, 1999
)
0.3
" These effects were more pronounced with dosing regimens launched before the time of oviposition."( Activity of 9-(S)-[3-hydroxy-2-(phosphonomethoxy)propyl]adenine against Schistosomiasis mansoni in mice.
Botros, S; Hammam, O; Holý, A; William, S; Zídek, Z, 2003
)
0.32
" This can be used as a starting point to investigate alternative administration routes or dosage forms and to examine the mechanism of intestinal absorption of PRZ."( Improvement of antischistosomal activity of praziquantel by incorporation into phosphatidylcholine-containing liposomes.
Costa, PI; Gremião, MP; Mourão, SC; Salgado, HR, 2005
)
0.33
" mansoni experimentally infected mice were treated at 9th week of infection with ART, PZQ or OX at an oral dosage of 300 mg kg(-1), 600 mg kg(-1) and 100 mg kg(-1), respectively."( Comparative studies on the pathological findings and mortality in Schistosoma mansoni infected mice after treatment with artesunate and the current antischistosomal drugs.
Chaiworaporn, R; Janecharut, T; Kitikoon, V; Maneerat, Y; Matsuda, H; Ramasoota, P; Rojekittikhun, W, 2005
)
0.33
" PZQ given as a dosage of 60 mg/kg (1 day, 3 x 20 mg/kg doses at 4-5 hour intervals) may be as effective as a dosage of 120 mg/kg (6 days, 20 mg/kg for each day split into 3 doses at 4-5 hour intervals)."( A randomized, double-blind, placebo-controlled trial of safety and efficacy of combined praziquantel and artemether treatment for acute schistosomiasis japonica in China.
Balen, J; Ellis, M; Gray, DJ; He, YK; Hou, XY; Li, YS; Luo, XS; McManus, DP; Williams, GM, 2008
)
0.35
" The implementation of this assay to the screening of a highly diverse academic chemical library of 14,300 molecules yielded, after secondary assays and generation of dose-response curves, the identification of two natural product inhibitors, cyanidin and delphinidin."( Identification by high-throughput screening of inhibitors of Schistosoma mansoni NAD(+) catabolizing enzyme.
Haiech, J; Hibert, M; Kellenberger, E; Kuhn, I; Lobstein, A; Muller-Steffner, H; Rognan, D; Said-Hassane, F; Schuber, F; Villa, P, 2010
)
0.36
" Male worms were more susceptible, producing a dose-response effect within a smaller exposition period than female worms."( Schistosoma mansoni: in vitro schistosomicidal activity of essential oil of Baccharis trimera (less) DC.
Allegretti, SM; de Carvalho, JE; de Oliveira, RN; de Ruiz, AL; Jeraldo, Vde L; Júnior, ÍM; Linhares, AX; Rehder, VL; Santos Oliveira, AS, 2012
)
0.38
"Further research will help find the optimal dosing regimen of both these drugs in children."( Drugs for treating Schistosoma mansoni infection.
Danso-Appiah, A; Donegan, S; Olliaro, PL; Sinclair, D; Utzinger, J, 2013
)
0.39
" Proper dosage adjustment of praziquantel by bodyweight can be difficult to achieve if accurate weighing scales are unavailable."( Validating the WHO dose pole in the Philippines for school-based mass drug administration of praziquantel for morbidity control of schistosomiasis.
Belizario, VY; Chua, PL; Erfe, JM; Naig, JR, 2013
)
0.39
" The quantal dose-response calculator (QDREC) constitutes a significant step in this direction."( The QDREC web server: determining dose-response characteristics of complex macroparasites in phenotypic drug screens.
Asarnow, D; Caffrey, CR; Rojo-Arreola, L; Singh, R; Suzuki, BM, 2015
)
0.42
" Praziquantel, dosed at 40 milligrams per kilogram bodyweight, is the drug of choice."( The Accuracy of Praziquantel Dose Poles for Mass Treatment of Schistosomiasis in School Girls in KwaZulu-Natal, South Africa.
Aurlund, CG; Baan, M; Gagai, S; Galappaththi-Arachchige, HN; Kjetland, EF; Taylor, M; van Lieshout, L; Vennervald, BJ, 2016
)
0.43
" In the current work, the therapeutic efficacy of different limonin dosing protocols was evaluated in experimentally infected mice harboring Schistosoma mansoni (Egyptian strain) juvenile or adult stages."( Dose-response relationship in Schistosoma mansoni juvenile and adult stages following limonin treatment in experimentally infected mice.
Abdallah, KF; Abou-Ouf, EA; Aly, NS; El-Kholy, AA; Eraky, MA; Hamdan, DI; Hammam, OA; Kishik, SM; Moharam, AF; Rashed, GA, 2016
)
0.43
" This XTT viability assay was validated for high throughput screening of compounds in schistosomula, and dose-response curves of compounds could be reproduced."( A high-throughput colorimetric assay for detection of Schistosoma mansoni viability based on the tetrazolium salt XTT.
Aguiar, PHN; Fernandes, NMGS; Mourão, MM; Zani, CL, 2017
)
0.46
" In silico models were used to predict murine dosing to recapitulate human conditions for OXA portal concentration and time course."( Addressing the oxamniquine in vitro-in vivo paradox to facilitate a new generation of anti-schistosome treatments.
Alwan, S; Cameron, MD; Khan, S; LoVerde, PT; McHardy, SF; Toth, K, 2023
)
0.91
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (3)

Assay IDTitleYearJournalArticle
AID1137146Antischistosomal activity against Schistosoma mansoni Puerto Rican infected mouse assessed as infected mouse at 140 mg/kg/day, through diet for 14 days1977Journal of medicinal chemistry, Dec, Volume: 20, Issue:12
Antischistosomal effects of 5-(2,4,5-trichlorophenyl)hydantoin and related compounds.
AID1137169Antischistosomal activity against Schistosoma mansoni Puerto Rican infected mouse assessed as reduction in live schistosomes at 140 mg/kg/day, through diet for 14 days1977Journal of medicinal chemistry, Dec, Volume: 20, Issue:12
Antischistosomal effects of 5-(2,4,5-trichlorophenyl)hydantoin and related compounds.
AID1137178Toxicity in mouse po dosed through diet for 14 days1977Journal of medicinal chemistry, Dec, Volume: 20, Issue:12
Antischistosomal effects of 5-(2,4,5-trichlorophenyl)hydantoin and related compounds.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (1,354)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990490 (36.19)18.7374
1990's209 (15.44)18.2507
2000's262 (19.35)29.6817
2010's319 (23.56)24.3611
2020's74 (5.47)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.38

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index12.38 (24.57)
Research Supply Index7.34 (2.92)
Research Growth Index4.55 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (12.38)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials65 (4.39%)5.53%
Reviews170 (11.47%)6.00%
Case Studies58 (3.91%)4.05%
Observational0 (0.00%)0.25%
Other1,189 (80.23%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]