ID Source | ID |
---|---|
PubMed CID | 11296583 |
CHEMBL ID | 2354444 |
CHEBI ID | 94770 |
SCHEMBL ID | 8323 |
MeSH ID | M0088759 |
Synonym |
---|
pirarubicin |
theprubicin |
pirarubicinum [latin] |
(2''r)-4'-o-tetrahydropyranyladriamycin |
thp-doxorubicin |
pirarubicine [french] |
pirarubicina [spanish] |
thp-adriamycin |
5,12-naphthacenedione, 10-((3-amino-2,3,6-trideoxy-4-o-(tetrahydro-2h-pyran-2-yl)-alpha-l-lyxo-hexopyranosyl)oxy)-7,8,9,10-tetrahydro-6,8,11-trihydroxy-8-(hydroxyacetyl)-1-methoxy-, (8s-cis)- |
pirarubicin [inn:jan] |
(8s,10s)-10-((3-amino-2,3,6-trideoxy-4-o-(2r-tetrahydro-2h-pyran-2-yl)-alpha-l-lyxo-hexopyranosyl)oxy)-8-glycoloyl-7,8,9,10-tetrahydro-6,8,11-trihydroxy-1-methoxy-5,12-naphthacenedione |
4'-o-tetrahydropyranyladriamycin |
1609rb |
4'-o-tetrahydropyranyldoxorubicin |
adriamycin, tetrahydropyranyl |
thp-adm |
72496-41-4 |
NCGC00167982-01 |
pirarubicine |
d58g680w0g , |
unii-d58g680w0g |
pirarubicinum |
pirarubicina |
tox21_112602 |
cas-72496-41-4 |
dtxsid2046755 , |
dtxcid0026755 |
S1393 |
BRD-K83794624-001-01-7 |
pirarubicin [who-dd] |
pirarubicin [jan] |
pirarubicin [mi] |
pirarubicin [inn] |
pirarubicin [mart.] |
(8s,10s)-10-((3-amino-2,3,6-trideoxy-4-o-(2r-tetrahydro-2h-pyran-2-yl)-.alpha.-l-lyxo-hexopyranosyl)oxy)-8-glycoloyl-7,8,9,10-tetrahydro-6,8,11-trihydroxy-1-methoxy-5,12-naphthacenedione |
HY-13725 |
SCHEMBL8323 |
tox21_112602_1 |
NCGC00344543-01 |
CHEMBL2354444 |
AKOS024464743 |
CHEBI:94770 |
(7s,9s)-7-[[(2r,4s,5s,6s)-4-amino-6-methyl-5-[[(2r)-2-oxanyl]oxy]-2-oxanyl]oxy]-6,9,11-trihydroxy-9-(2-hydroxy-1-oxoethyl)-4-methoxy-8,10-dihydro-7h-tetracene-5,12-dione |
SW219079-1 |
DB11616 |
(7s,9s)-7-[(2r,4s,5s,6s)-4-amino-6-methyl-5-[(2r)-oxan-2-yl]oxyoxan-2-yl]oxy-6,9,11-trihydroxy-9-(2-hydroxyacetyl)-4-methoxy-8,10-dihydro-7h-tetracene-5,12-dione |
(8s,10s)-10-(((2r,4s,5s,6s)-4-amino-6-methyl-5-(((r)-tetrahydro-2h-pyran-2-yl)oxy)tetrahydro-2h-pyran-2-yl)oxy)-6,8,11-trihydroxy-8-(2-hydroxyacetyl)-1-methoxy-7,8,9,10-tetrahydrotetracene-5,12-dione |
CCG-270279 |
Pirarubicin (PIRA) is a semi-synthetic anthracycline derivative that is reported to have lesser toxicity and better clinical outcomes as compared to its parental form doxorubic inDOX. Pirarubi is a widely used antitumor drug in clinical practice, but its cardiotoxicity limits its use.
Pirarubicin (PIRA) has been shown to have improved potency with less cardiac toxicity in several phase I and II clinical trials in Japan and Europe.
Excerpt | Reference |
---|---|
"Pirarubicin was treated with various kinds of aryl aldehydes." | ( N-salicylidene derivatives of pirarubicin. Ajito, K; Ikeda, D; Komuro, K; Kondo, S; Nosaka, C; Takeuchi, T; Wako, N, 1989) |
Pirarubicin is characterised by strong haematological toxicity, which has been shown to be correlated with pharmacokinetic parameters. The percentage of survival of granulocytes was significantly correlated with the AUC values for doxorubsicin and doxorsicinol.
Excerpt | Reference |
---|---|
" A relationship was observed between some pharmacokinetic parameters and the toxic effects of the drug: the percentage of survival of granulocytes was significantly correlated with the AUC values for doxorubicin and doxorubicinol, whereas that of platelets was significantly correlated with the AUC values for pirarubicin and pirarubicinol." | ( A pharmacokinetic and pharmacodynamic study of the new anthracycline pirarubicin in breast cancer patients. Hérait, P; Monnier, A; Poutignat, N; Robert, J, 1991) |
" Each molecule is characterized by original metabolic and pharmacokinetic features, which can be compared to those of the reference anthracyclines, doxorubicin and daunorubicin." | ( [Pharmacokinetics of new anthracyclines]. Robert, J, 1988) |
" This time, a pharmacokinetic study of THP-ADM was performed and the following characteristics of this agent were clarified." | ( [Pharmacokinetic studies on THP-ADM (tetrahydropyranyl adriamycin)]. Majima, H, 1987) |
" Pharmacokinetic analysis of the plasma level of THP by the simulation according to a three-compartment open model provided large values of apparent volume of distribution in the tissue compartment." | ( [Pharmacokinetics and disposition of a new anticancer antibiotic (2''R)-4'-O-tetrahydropyranyladriamycin in rats. Distribution and excretion after a single administration]. Esumi, Y; Fujigaki, M; Iguchi, H; Nishio, M; Takaichi, M; Tone, H; Tsutsumi, S; Yokoshima, T, 1986) |
"The pharmacokinetic properties of THP and ADM were comparatively studied in the same patients with various cancers." | ( [Comparative studies on the pharmacokinetics between THP and adriamycin in the same patients]. Imamura, Y; Kawamura, K; Koyama, Y; Matsumoto, A; Murata, S; Nakajima, O; Shomura, T, 1986) |
" This time, a pharmacokinetic study of THP-ADM was performed and the following characteristics of this agent were clarified." | ( [Pharmacokinetic studies of THP-ADM (tetrahydropyranyl adriamycin)]. Iguchi, H; Majima, H; Tone, H, 1986) |
"15 min; terminal elimination half-life (t1/2 gamma), 13." | ( Pharmacokinetics of 4'-O-tetrahydropyranyladriamycin given on a weekly schedule in patients with advanced breast cancer. Baur, M; Dittrich, C; Greifenberg, B; Heberle, U; Mader, RM; Schlappack, O; Steger, GG; Zilg, H, 1995) |
" Pirarubicin is characterised by strong haematological toxicity, which has been shown to be correlated with pharmacokinetic parameters, especially the area under the time-concentration curve." | ( A limited sampling strategy for the study of pirarubicin pharmacokinetics in humans. Galeani, A; Iliadis, A; Leca, FR; Marchiset-Leca, D; Noble, A, 1995) |
"The pharmacokinetic monitoring of anthracycline-containing regimens is warranted because of the important toxicity of these drugs and because pharmacokinetic-pharmacodynamic relationships have been clearly established." | ( Pharmacokinetics and metabolism of pirarubicin in humans: correlation with pharmacodynamics. Catalin, J; Galeani, A; Leca, FR; Marchiset-Leca, D; Noble, A, 1995) |
" THP concentration was measured by HPLC, and the pharmacokinetic parameters of this drug were estimated in plasma and CSF." | ( Pharmacokinetics of intra-arterially administered pirarubicin in plasma and cerebrospinal fluid of patients with glioma. Hori, S; Mori, T; Morikawa, N; Takeyama, M, 1998) |
"The objective of the present study was to evaluate the relationship between the pharmacokinetic parameters of pirarubicin and of its metabolite doxorubicin measured in plasma and whole blood, and the hematologic toxicity of this drug, in order to evaluate the predictability of changes in white blood cells (WBC) by single measurement of drug concentrations." | ( Pharmacokinetic-pharmacodynamic relationships between pirarubicin exposure and hematotoxicity: clinical application using only one blood sample. Catalin, J; Galeani, A; Leca, FR; Marchiset-Leca, D; Noble, A, 1998) |
" Comparative studies on pharmacokinetic and biodistribution behaviors between L-THP and commercialized THP injection were performed in normal mice through intravenous administration." | ( Characterization and pharmacokinetics of a novel pirarubicin liposome powder. Chen, X; Cong, W; Gao, R; Liu, Q; Lu, J; Luo, G; Wang, Y, 2010) |
BD regimen combined with cyclophosphamide and pirarubicin chemotherapy can improve the response rate of patients with relapse/refractory multiple myeloma.
Excerpt | Reference |
---|---|
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs." | ( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019) |
Pirarubicin (THP) used with this dosage and schedule has no activity in advanced pancreatic carcinoma.
Class | Description |
---|---|
anthracycline | Anthracyclines are polyketides that have a tetrahydronaphthacenedione ring structure attached by a glycosidic linkage to the amino sugar daunosamine. |
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] |
Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Luciferase | Photinus pyralis (common eastern firefly) | Potency | 38.9018 | 0.0072 | 15.7588 | 89.3584 | AID1224835 |
acetylcholinesterase | Homo sapiens (human) | Potency | 17.3768 | 0.0025 | 41.7960 | 15,848.9004 | AID1347395 |
hypoxia-inducible factor 1 alpha subunit | Homo sapiens (human) | Potency | 20.6767 | 3.1890 | 29.8841 | 59.4836 | AID1224846; AID1224894 |
RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 11.8832 | 0.0060 | 38.0041 | 19,952.5996 | AID1159521 |
Fumarate hydratase | Homo sapiens (human) | Potency | 2.5119 | 0.0030 | 8.7949 | 48.0869 | AID1347053 |
TDP1 protein | Homo sapiens (human) | Potency | 0.2617 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
GLI family zinc finger 3 | Homo sapiens (human) | Potency | 0.0302 | 0.0007 | 14.5928 | 83.7951 | AID1259369; AID1259392 |
AR protein | Homo sapiens (human) | Potency | 5.3129 | 0.0002 | 21.2231 | 8,912.5098 | AID1259243; AID1259247; AID743035; AID743036; AID743042; AID743053; AID743054; AID743063 |
caspase 7, apoptosis-related cysteine protease | Homo sapiens (human) | Potency | 2.3710 | 0.0133 | 26.9810 | 70.7614 | AID1346978 |
estrogen receptor 2 (ER beta) | Homo sapiens (human) | Potency | 26.6032 | 0.0006 | 57.9133 | 22,387.1992 | AID1259378 |
nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 0.7085 | 0.0010 | 22.6508 | 76.6163 | AID1224838; AID1224893 |
progesterone receptor | Homo sapiens (human) | Potency | 12.8285 | 0.0004 | 17.9460 | 75.1148 | AID1346784; AID1346795; AID1347036 |
cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 4.7460 | 0.0123 | 7.9835 | 43.2770 | AID1346984; AID1645841 |
glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 2.3839 | 0.0002 | 14.3764 | 60.0339 | AID720691; AID720692; AID720719 |
retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 0.0119 | 0.0030 | 41.6115 | 22,387.1992 | AID1159552 |
retinoid X nuclear receptor alpha | Homo sapiens (human) | Potency | 11.5344 | 0.0008 | 17.5051 | 59.3239 | AID1159531 |
estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 2.2995 | 0.0015 | 30.6073 | 15,848.9004 | AID1224841; AID1224842; AID1224848; AID1224849; AID1259401; AID1259403 |
farnesoid X nuclear receptor | Homo sapiens (human) | Potency | 4.5325 | 0.3758 | 27.4851 | 61.6524 | AID743217; AID743220 |
pregnane X nuclear receptor | Homo sapiens (human) | Potency | 12.5893 | 0.0054 | 28.0263 | 1,258.9301 | AID1346985 |
estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 6.7643 | 0.0002 | 29.3054 | 16,493.5996 | AID1259244; AID1259248; AID743069; AID743075; AID743077; AID743079; AID743080; AID743091 |
G | Vesicular stomatitis virus | Potency | 12.3018 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
polyprotein | Zika virus | Potency | 2.5119 | 0.0030 | 8.7949 | 48.0869 | AID1347053 |
peroxisome proliferator-activated receptor delta | Homo sapiens (human) | Potency | 7.4972 | 0.0010 | 24.5048 | 61.6448 | AID743215 |
peroxisome proliferator activated receptor gamma | Homo sapiens (human) | Potency | 16.3939 | 0.0010 | 19.4141 | 70.9645 | AID743094; AID743191 |
vitamin D (1,25- dihydroxyvitamin D3) receptor | Homo sapiens (human) | Potency | 10.7014 | 0.0237 | 23.2282 | 63.5986 | AID743222; AID743223 |
caspase-3 | Homo sapiens (human) | Potency | 2.3710 | 0.0133 | 26.9810 | 70.7614 | AID1346978 |
aryl hydrocarbon receptor | Homo sapiens (human) | Potency | 2.3710 | 0.0007 | 23.0674 | 1,258.9301 | AID743085 |
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_a | Homo sapiens (human) | Potency | 3.3491 | 0.0017 | 23.8393 | 78.1014 | AID743083 |
activating transcription factor 6 | Homo sapiens (human) | Potency | 30.1065 | 0.1434 | 27.6121 | 59.8106 | AID1159516 |
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_a | Homo sapiens (human) | Potency | 30.1065 | 19.7391 | 45.9784 | 64.9432 | AID1159509 |
v-jun sarcoma virus 17 oncogene homolog (avian) | Homo sapiens (human) | Potency | 0.6740 | 0.0578 | 21.1097 | 61.2679 | AID1159526; AID1159528 |
nuclear receptor subfamily 1, group I, member 2 | Rattus norvegicus (Norway rat) | Potency | 12.5893 | 0.1000 | 9.1916 | 31.6228 | AID1346983 |
Histone H2A.x | Cricetulus griseus (Chinese hamster) | Potency | 4.4720 | 0.0391 | 47.5451 | 146.8240 | AID1224845; AID1224896 |
thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 0.9709 | 0.0003 | 23.4451 | 159.6830 | AID743065; AID743067 |
histone deacetylase 9 isoform 3 | Homo sapiens (human) | Potency | 11.8832 | 0.0376 | 17.0823 | 61.1927 | AID1259364; AID1259388 |
nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 0.5955 | 0.0006 | 27.2152 | 1,122.0200 | AID743219 |
Voltage-dependent calcium channel gamma-2 subunit | Mus musculus (house mouse) | Potency | 2.6603 | 0.0015 | 57.7890 | 15,848.9004 | AID1259244 |
Interferon beta | Homo sapiens (human) | Potency | 12.3018 | 0.0033 | 9.1582 | 39.8107 | AID1645842 |
HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 12.3018 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
Cellular tumor antigen p53 | Homo sapiens (human) | Potency | 2.9901 | 0.0023 | 19.5956 | 74.0614 | AID651631; AID720552 |
Glutamate receptor 2 | Rattus norvegicus (Norway rat) | Potency | 2.6603 | 0.0015 | 51.7393 | 15,848.9004 | AID1259244 |
Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 12.3018 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
ATPase family AAA domain-containing protein 5 | Homo sapiens (human) | Potency | 2.5157 | 0.0119 | 17.9420 | 71.5630 | AID651632; AID720516 |
Ataxin-2 | Homo sapiens (human) | Potency | 2.3710 | 0.0119 | 12.2221 | 68.7989 | AID651632 |
cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 12.3018 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID21036 | Tested for the partition coefficient between water and n-octanol. | 1990 | Journal of medicinal chemistry, Jan, Volume: 33, Issue:1 | Structure-activity relationship of anthracyclines in vitro. |
AID1079948 | Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source] | |||
AID1079937 | Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source] | |||
AID83957 | Tested for the cytotoxicity (continuous incubation) against human colon tumor cell lines (HT 29) determined by clonogenic assay. | 1990 | Journal of medicinal chemistry, Jan, Volume: 33, Issue:1 | Structure-activity relationship of anthracyclines in vitro. |
AID1079940 | Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source] | |||
AID1079945 | Animal toxicity known. [column 'TOXIC' in source] | |||
AID83956 | Tested for the cytotoxicity(1 hour incubation) against human colon tumor cell lines (HT 29). | 1990 | Journal of medicinal chemistry, Jan, Volume: 33, Issue:1 | Structure-activity relationship of anthracyclines in vitro. |
AID1079947 | Comments (NB not yet translated). [column 'COMMENTAIRES' in source] | |||
AID1079943 | Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source] | |||
AID1079944 | Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source] | |||
AID1079939 | Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source] | |||
AID101085 | Tested for the cytotoxicity(1 hour incubation) against L1210 leukemia cells. | 1990 | Journal of medicinal chemistry, Jan, Volume: 33, Issue:1 | Structure-activity relationship of anthracyclines in vitro. |
AID1079942 | Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source] | |||
AID101086 | Tested for the cytotoxicity (continuous incubation) against L1210 leukemia cells determined by clonogenic assay. | 1990 | Journal of medicinal chemistry, Jan, Volume: 33, Issue:1 | Structure-activity relationship of anthracyclines in vitro. |
AID54463 | Tested for the binding affinity for DNA by intercalation between adjacent base pairs of the helix. | 1990 | Journal of medicinal chemistry, Jan, Volume: 33, Issue:1 | Structure-activity relationship of anthracyclines in vitro. |
AID1079932 | Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source] | |||
AID1079934 | Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source] | |||
AID1079935 | Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source] | |||
AID50756 | Tested for the cytotoxicity(1 hour incubation) against human colon tumor cell lines colon 4). | 1990 | Journal of medicinal chemistry, Jan, Volume: 33, Issue:1 | Structure-activity relationship of anthracyclines in vitro. |
AID1079946 | Presence of at least one case with successful reintroduction. [column 'REINT' in source] | |||
AID1079936 | Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source] | |||
AID1546435 | Antiproliferative activity against mouse L5178Y cells assessed as reduction in cell viability | 2020 | Bioorganic & medicinal chemistry letters, 01-01, Volume: 30, Issue:1 | Identification of HUHS190, a human naftopidil metabolite, as a novel anti-bladder cancer drug. |
AID1546436 | Antitumor activity against mouse MB49 cells xenografted in C57BL/6 mouse bladder cancer model assessed as death rate at 1 mg/ml dosed via intravesical instillation through catheter for 2 hrs and measured after 28 days relative to control | 2020 | Bioorganic & medicinal chemistry letters, 01-01, Volume: 30, Issue:1 | Identification of HUHS190, a human naftopidil metabolite, as a novel anti-bladder cancer drug. |
AID1079933 | Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is | |||
AID1079938 | Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source] | |||
AID1079949 | Proposed mechanism(s) of liver damage. [column 'MEC' in source] | |||
AID50757 | Tested for the cytotoxicity (continuous incubation) against human colon tumor cell lines (colon 4)determined by clonogenic assay. | 1990 | Journal of medicinal chemistry, Jan, Volume: 33, Issue:1 | Structure-activity relationship of anthracyclines in vitro. |
AID1546434 | Antiproliferative activity against C3H mouse MBT2 cells assessed as reduction in cell viability | 2020 | Bioorganic & medicinal chemistry letters, 01-01, Volume: 30, Issue:1 | Identification of HUHS190, a human naftopidil metabolite, as a novel anti-bladder cancer drug. |
AID1546433 | Antiproliferative activity against mouse MB49 cells assessed as reduction in cell viability after 72 hrs by WST-8 assay | 2020 | Bioorganic & medicinal chemistry letters, 01-01, Volume: 30, Issue:1 | Identification of HUHS190, a human naftopidil metabolite, as a novel anti-bladder cancer drug. |
AID1079931 | Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source] | |||
AID1079941 | Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source] | |||
AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347119 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347111 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347122 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347114 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347424 | RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46 | Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
AID1347112 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347115 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347123 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347129 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
AID1347117 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347113 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347127 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347121 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347128 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347126 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347116 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347425 | Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46 | Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
AID1347118 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347407 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
AID1347125 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347110 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347124 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347109 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 119 (15.24) | 18.7374 |
1990's | 288 (36.88) | 18.2507 |
2000's | 156 (19.97) | 29.6817 |
2010's | 163 (20.87) | 24.3611 |
2020's | 55 (7.04) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 133 (16.42%) | 5.53% |
Reviews | 24 (2.96%) | 6.00% |
Case Studies | 135 (16.67%) | 4.05% |
Observational | 4 (0.49%) | 0.25% |
Other | 514 (63.46%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
---|---|---|---|---|---|---|---|
Sensitivity Detection and Drug Resistance Mechanism of Breast Cancer Therapeutic Drugs Based on Organ-like Culture[NCT03925233] | 300 participants (Anticipated) | Observational | 2019-01-02 | Enrolling by invitation | |||
A Multicenter, Randomized, Double-blind, Prospective Study to Evaluate the Efficacy and Safety of Vincristine, Dactinomycin/Cyclophosphamide Combination Therapy Combined With Liposomal Doxorubicin/Doxorubicin/Pharmorubicin/Pirarubicin in 0.5-14 Year Old C[NCT03892330] | Phase 4 | 120 participants (Anticipated) | Interventional | 2019-06-01 | Not yet recruiting | ||
A Multicenter, Randomised, Open-label Phase II Study to Evaluate the Efficacy and Safety of Adjuvant Chemotherapy for Triple Negative Breast Cancer Patients With Residual Disease After Platinum-based Neoadjuvant Chemotherapy[NCT04437160] | Phase 2 | 286 participants (Anticipated) | Interventional | 2020-02-01 | Recruiting | ||
Comparative Analysis of the Efficacies of AT and AC-T Regimens in Neoadjuvant Chemotherapy of Breast Cancer[NCT02613026] | Phase 3 | 104 participants (Actual) | Interventional | 2009-07-31 | Completed | ||
Modified BFM-95 Regimen for the Treatment of Newly Diagnosed T-lymphoblastic Lymphoma in Adults:a Prospective Phase II Study[NCT02396043] | Phase 2 | 50 participants (Anticipated) | Interventional | 2015-03-31 | Recruiting | ||
Peking University First Hospital[NCT02740426] | Phase 2 | 200 participants (Anticipated) | Interventional | 2016-08-31 | Recruiting | ||
Liver Resection Versus Transarterial Chemoembolization for the Treatment of Intermediate-stage Hepatocellular Carcinoma: a Prospective Non-randomized Trial[NCT02755311] | Phase 3 | 198 participants (Anticipated) | Interventional | 2014-03-31 | Recruiting | ||
Systemic Chemotherapy VersusTranscatheter Arterial Chemoembolization As Palliative Chemotherapy in Patients With Advanced Hepatocellular Carcinoma(HCC)[NCT02585479] | Phase 2/Phase 3 | 0 participants (Actual) | Interventional | 2015-10-31 | Withdrawn(stopped due to It doesn't meet the requirements of randomized trials) | ||
[NCT02547350] | Phase 2 | 200 participants (Anticipated) | Interventional | 2015-09-30 | Not yet recruiting | ||
Marched Pair Study of the Standard Chemotherapy 4doxorubicin Plus Cyclophosphamide(AC) 60 + 4 Docetaxel Protocol Versus 4 PLD C35+4 Docetaxel in Neoadjuvant Chemotherapy of Breast Cancer[NCT02953184] | Phase 2 | 160 participants (Anticipated) | Interventional | 2016-11-30 | Recruiting | ||
[NCT02923557] | Phase 2 | 200 participants (Anticipated) | Interventional | 2016-11-30 | Recruiting | ||
Adjuvant AC Followed by Albumin-bound Paclitaxel Versus AC Followed by Taxanes in Breast Cancer: a Prospective, Multi-center, Real-world Study[NCT05287308] | 500 participants (Anticipated) | Interventional | 2022-03-31 | Not yet recruiting | |||
Study of Efficacy of PAD-regimen(Bortezomib,Pirarubicin and Dexamethasone) and TAD-regimen(Thalidomide,Pirarubicin and Dexamethasone) in Newly Diagnosed Multiple Myeloma,Influence in Concentration of Bone Metabolites,and the Relations With Different Cytog[NCT01249690] | Phase 4 | 100 participants (Anticipated) | Interventional | 2010-06-30 | Recruiting | ||
The Efficacy and Safety of Doxorubicin Hydrochloride Liposome Injection Plus Cyclophosphamide Compared to Pirarubicin Plus Cyclophosphamide as Neoadjuvant Chemotherapy in Locally Advanced Breast Cancer :a Randomised Multicentre, Open-label Trial[NCT02903524] | Phase 4 | 300 participants (Anticipated) | Interventional | 2016-09-30 | Recruiting | ||
Phase 2 Study of Applying Pediatric Regimens to Younger Adult Patients With BCR-ABL-Negative Acute Lymphoblastic Leukemia[NCT00131053] | Phase 2 | 120 participants (Anticipated) | Interventional | 2002-09-30 | Recruiting | ||
An Open-label,Multicenter Randomised Study of CTOP/ITE/MTX Compared With CHOP as the First-line Therapy for the New Diagnosed Young Patients With T Cell Non-hodgkin Lymphoma[NCT01746992] | Phase 4 | 200 participants (Anticipated) | Interventional | 2012-09-30 | Active, not recruiting | ||
Prospective Randomized Phase II Trial: Single Instillation Versus Long-term Prophylactic Intravesical Instillation of Pirarubicin in the Prevention of Bladder Recurrence After Nephroureterectomy for Primary Upper Tract Urothelial Carcinoma[NCT03030157] | Phase 2 | 220 participants (Anticipated) | Interventional | 2017-01-31 | Recruiting | ||
Combine Transcatheter Arterial Embolization and Radiofrequency Ablation Versus Transcatheter Arterial Embolization Alone for Hepatocellular Carcinoma With Portal Vein Tumor Thrombus[NCT02301091] | Phase 3 | 240 participants (Anticipated) | Interventional | 2014-10-31 | Recruiting | ||
Single-center, Open, Non-randomized, Phase II Prospective Study of Apatinib Combined With Chemotherapy in the Treatment of Unresectable Soft Tissue Sarcoma[NCT04126811] | Phase 2 | 120 participants (Anticipated) | Interventional | 2019-06-01 | Recruiting | ||
Comparing the Effectiveness and Toxicity for Locally Advanced, Unresectable or Metastatic Soft-tissue Sarcoma Patients Who Had Received Total Dose of Anthracycline Antibiotics More Than 300mg/m2 With Pegylated Liposomal Doxorubicin Versus Pirarubicin Plus[NCT03342300] | Phase 2/Phase 3 | 0 participants (Actual) | Interventional | 2017-11-06 | Withdrawn(stopped due to No participants enrolled) | ||
[information is prepared from clinicaltrials.gov, extracted Sep-2024] |