Page last updated: 2024-12-07

norcantharidin

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Description

Norcantharidin is a potent and selective inhibitor of protein phosphatase 2A (PP2A). PP2A is a ubiquitous serine/threonine phosphatase that plays a crucial role in regulating a wide range of cellular processes, including cell growth, proliferation, and differentiation. Norcantharidin has been shown to have anti-cancer activity in vitro and in vivo, and is currently being investigated as a potential cancer therapeutic. Norcantharidin is synthesized through a multi-step process involving the extraction and modification of cantharidin, a naturally occurring compound found in blister beetles. The molecule's unique structure allows it to bind to and inhibit PP2A, thus disrupting the normal function of this essential enzyme. Researchers are studying norcantharidin to understand its potential therapeutic applications in cancer treatment and to further elucidate the role of PP2A in various cellular processes.'

norcantharidin: structure given in first source; RN given refers to cpds without isomeric designation [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID93004
CHEMBL ID8327
CHEBI ID197221
SCHEMBL ID177729
MeSH IDM0190238

Synonyms (103)

Synonym
DIVK1C_007000
norcantharidin
EU-0100830
norcantharidin, solid
3,6-endooxyphthalic anhydride, hexahydro-
4,7-epoxyisobenzofuran-1,3-dione, hexahydro-
nsc 14003
phthalic anhydride, hexahydro-3,6-endoxo-
endothall anhydride
7-oxabicyclo(2.2.1)heptane-2,3-dicarboxylic anhydride
nsc59023
SPECTRUM_001667
phthalic anhydride,6-endoxo-
4,3-dione, hexahydro-
wln: t c555 a ao dvovtj
3, hexahydro-
nsc14003
7-oxabicyclo[2.2.1]heptane-2,3-dicarboxylic anhydride
3,6-endoxohexahydrophthalic anhydride
5442-12-6
BSPBIO_003327
SPECTRUM5_001514
LOPAC0_000830
nsc148536
51154-98-4
nsc-148536
NCGC00094161-02
NCGC00094161-04
NCGC00094161-03
NCI60_001019
KBIO1_001944
KBIO2_004715
KBIOGR_001122
KBIO3_002547
KBIO2_002147
KBIOSS_002147
KBIO2_007283
SPECPLUS_000904
SPBIO_001606
SPECTRUM2_001683
SPECTRUM3_001634
SPECTRUM4_000601
SPECTRUM1504153
NCGC00094161-06
NCGC00094161-05
NCGC00094161-01
exo-7-oxa-bicyclo(2.2.1)-heptane-2,3-dicarboxylic anhydride
MLS002153470
smr000326693
hexahydro-4,7-epoxy-2-benzofuran-1,3-dione
STK424286
NCGC00015756-03
N 8784
NCGC00015756-09
demethyl-cantharidin
CHEMBL8327
4,10-dioxatricyclo[5.2.1.02,6]decane-3,5-dione
CHEBI:197221
AKOS003267901
HMS3262F21
4,10-dioxatricyclo[5.2.1.0<2,6>]decane-3,5-dione
S3759
CCG-39454
NCGC00015756-07
NCGC00015756-06
NCGC00015756-05
NCGC00015756-08
NCGC00015756-04
FT-0614776
FT-0621477
FT-0626378
LP00830
HMS3370H07
AKOS022167759
SCHEMBL177729
tox21_500830
NCGC00261515-01
4,10-dioxa-tricyclo[5.2.1.02,6]decane-3,5-dione
JAABVEXCGCXWRR-UHFFFAOYSA-N
norcantharadine
mfcd00213361
3,6-endoxohexahydrophthalic anhydride, exo isomer
hexahydro-4,7-epoxyisobenzofuran-1,3-dione
SR-01000076037-1
sr-01000076037
BCP25426
exo-cis-hexahydro-4,7-epoxyisobenzofuran-1,3-dione; endothall anhydride
HY-N0585
(rac)-norcantharidin
timtec-bb sbb005955;4,7-epoxyisobenzofuran-1,3-dione, hexahydro-;4,10-dioxatricyclo[5.2.1.0(2,6)]decane-3,5-dione
BCP09826
Q15425762
BRD-A66914119-001-04-0
FS-4623
SDCCGSBI-0050807.P003
NCGC00015756-14
(+/-)-norcantharidin
(+/-)-nctd
CS-0009119
YSCH0101
DTXSID30884158
3-(5'-(4-(diphenylamino)phenyl)-[2,2'-bithiophen]-5-yl)cyclohex-2-enone
4,10-dioxatricyclo[5.2.1.0(2,6)]decane-3,5-dione; 7-oxabicyclo[2.2.1]heptane-2,3-dicarboxylic anhydride

Research Excerpts

Overview

Norcantharidin (NCTD) is a powerful antitumor agent with multiple bioactivities. It has anti-proliferative, anti-inflammatory, and anti-fibrosis properties. It is an active ingredient of the traditional Chinese medicine Mylabris.

ExcerptReferenceRelevance
"Norcantharidin (NCTD) is a powerful antitumor agent with multiple bioactivities."( Norcantharidin Induces Immunogenic Cell Death of Bladder Cancer Cells through Promoting Autophagy in Acidic Culture.
Hu, Z; Li, H; Li, J; Mo, L; Su, B; Xu, L; Zhao, C; Zhao, Z, 2022
)
2.89
"Norcantharidin (NCTD) is a demethylated derivative of cantharidin demonstrated to have anti-proliferative, anti-inflammatory, and anti-fibrosis properties. "( Norcantharidin attenuates epidermal growth factor-induced proliferation, EMT and motility in ARPE-19 cells by modulating the AKT/snail/E-cadherin axis.
Chen, YS; Chien, HW; Chiou, HL; Hsieh, YH; Wang, K; Yang, SF, 2022
)
3.61
"Norcantharidin (NCTD) is a demethylated derivative of cantharidin (CTD), the main anticancer active ingredient isolated from traditional Chinese medicine Mylabris. "( Review targeted drug delivery systems for norcantharidin in cancer therapy.
Cheng, JX; Fan, Y; Guo, DY; Shi, YJ; Sun, J; Tian, H; Zhai, BT; Zhang, XF; Zou, JB, 2022
)
2.43
"Norcantharidin is a cantharidin demethylated analog with antitumor effects in many tumors, including cholangiocarcinoma. "( Autophagy Suppression Accelerates Apoptosis Induced by Norcantharidin in Cholangiocarcinoma.
Guo, H; Jiang, W; Li, C; Li, X; Tian, Q; Wang, Y; Xiong, X, 2020
)
2.25
"Norcantharidin (NCTD) is a potential anti-renal interstitial fibrotic drug. "( Protein Phosphatase 2A Inhibiting β-Catenin Phosphorylation Contributes Critically to the Anti-renal Interstitial Fibrotic Effect of Norcantharidin.
Li, Y; Tang, C; Wen, L; Xiao, Z; Yin, D; Zeng, D; Zhou, X, 2020
)
2.2
"Norcantharidin (NCTD) is a structural modifier of CTD."( Norcantharidin: research advances in pharmaceutical activities and derivatives in recent years.
Cao, Z; Guo, C; Li, Y; Ren, Y; Song, X; Tan, L; Wang, M; Zhou, J, 2020
)
2.72
"Norcantharidin (NCTD) is a demethylated derivative of cantharidin with antitumor properties which is an active ingredient of the traditional Chinese medicine Mylabris."( Norcantharidin counteracts acquired everolimus resistance in renal cell carcinoma by dual inhibition of mammalian target of rapamycin complex 1 and complex 2 pathways in Vitro.
Cai, X; Chen, S; Chen, X; Chen, Y; Deng, T; Huang, X; Li, H; Li, J; Mo, L; Zheng, D, 2022
)
2.89
"Norcantharidin (NCTD) is a promising antitumor drug with low toxicity. "( Norcantharidin enhances antitumor immunity of GM-CSF prostate cancer cells vaccine by inducing apoptosis of regulatory T cells.
Gao, J; Hu, Z; Li, H; Li, J; Mo, L; Shi, X; Wei, L; Zhang, X; Zheng, D, 2018
)
3.37
"Norcantharidin (NCTD) is a traditional Chinese medicine used in the treatment of many types of cancer, to which patients do not develop resistance."( Norcantharidin reverses cisplatin resistance and inhibits the epithelial mesenchymal transition of human non‑small lung cancer cells by regulating the YAP pathway.
Gao, Y; Guo, J; Jin, D; Shao, C; Wang, D; Wu, Y, 2018
)
2.64
"Norcantharidin is an important substitute of cantharidin and has similar insecticidal activities to cantharidin."( Effects of Cantharidin and Norcantharidin on Larval Feeding and Adult Oviposition Preferences of the Diamondback Moth (Lepidoptera: Plutellidae).
Li, YF; Sun, H; Xi, N; Zhang, Y, 2019
)
1.53
"Norcantharidin (NCTD) is an effective anti-tumor compound with severe nephrotoxicity."( Synthesis and anti-metastasis activities of norcantharidin-conjugated carboxymethyl chitosan as a novel drug delivery system.
Chi, J; Han, B; Jiang, Z; Liu, W; Peng, Y; Qiao, J, 2019
)
1.5
"Norcantharidin (NCTD) is a promising agent for inhibiting renal interstitial fibrosis."( Norcantharidin inhibits renal interstitial fibrosis by blocking the tubular epithelial-mesenchymal transition.
Duan, S; Hou, T; Li, H; Li, J; Li, Y; Liu, F; Liu, H; Liu, Y; Peng, Y; Sun, L; Sun, Y; Wang, M; Wang, S; Xi, Y; Xiao, L; You, Y, 2013
)
2.55
"Norcantharidin (NCTD) is an efficacious anti-cancer drug that has been used in China for many years, but its underlying mechanism of action is still not fully understood. "( Norcantharidin Suppresses Colon Cancer Cell Epithelial-Mesenchymal Transition by Inhibiting the αvβ6-ERK-Ets1 Signaling Pathway.
Agrez, M; Gao, C; Gao, H; He, Z; Li, Z; Lin, P; Niu, J; Niu, W; Niu, Z; Peng, C; Wang, J; Xu, Z; Zhang, Z, 2016
)
3.32
"Norcantharidin (NCTD) is a Chinese FDA approved, chemically synthesized drug for cancer treatment. "( Norcantharidin Inhibits cell growth by suppressing the expression and phosphorylation of both EGFR and c-Met in human colon cancer cells.
Cui, Y; He, Y; Liu, M; Ma, H; Qiu, P; Tang, Y; Wang, S; Xu, H; Xu, L; Zeng, X; Zhang, L; Zhang, M, 2017
)
3.34
"Norcantharidin (NCTD) is a small molecule toxin."( [Preparation of the immunotoxin 2E8-norcantharidin and its targeting killing effect in vitro].
Li, LX; Luo, CF; Qian, BQ; Shen, HQ; Tang, YM; Zhang, HZ, 2008
)
1.34
"Norcantharidin (NCTD) is a small-molecule metastasis inhibitor without renal toxicity derived from a renal toxic compound cantharidin, which is found in blister beetles (Mylabris phalerata Pall.), commonly used in traditional Chinese medicine. "( A small-molecule metastasis inhibitor, norcantharidin, downregulates matrix metalloproteinase-9 expression by inhibiting Sp1 transcriptional activity in colorectal cancer cells.
Chang, WM; Chen, YJ; Jang, YH; Kuo, CD; Lee, CY; Liao, HF; Liu, YW, 2009
)
2.06
"Norcantharidin (NCTD) is a potential anti-cancer agent that inhibits proliferation and induces cell death through regulation of mitogen-activated protein kinases (MAPK). "( Norcantharidin induces cell cycle arrest and inhibits progression of human leukemic Jurkat T cells through mitogen-activated protein kinase-mediated regulation of interleukin-2 production.
Chen, YJ; Chou, CH; Kuo, CD; Liao, HF; Wang, FW, 2011
)
3.25
"Norcantharidin (NCTD) is an anticancer drug routinely used against hepatoma in China. "( Norcantharidin-induced apoptosis is via the extracellular signal-regulated kinase and c-Jun-NH2-terminal kinase signaling pathways in human hepatoma HepG2 cells.
Chen, JC; Chen, YN; Cheng, CC; Hsu, SL; Tsauer, W, 2003
)
3.2
"Norcantharidin (3) is a potent PP1 (IC(50)=9.0+/-1.4 microM) and PP2A (IC(50)=3.0+/-0.4 microM) inhibitor with 3-fold PP2A selectivity and induces growth inhibition (GI(50) approximately 45 microM) across a range of human cancer cell lines including those of colorectal (HT29, SW480), breast (MCF-7), ovarian (A2780), lung (H460), skin (A431), prostate (DU145), neuroblastoma (BE2-C), and glioblastoma (SJ-G2) origin. "( Heterocyclic substituted cantharidin and norcantharidin analogues--synthesis, protein phosphatase (1 and 2A) inhibition, and anti-cancer activity.
Ackland, SP; Gilbert, J; Hill, TA; McCluskey, A; Sakoff, JA; Sauer, B; Stewart, SG, 2007
)
2.05
"Norcantharidin (NCTD) is a synthetic analog of cantharidin. "( The preliminary observation on immunosuppressive effect of norcantharidin in mice.
Piao, XH; Wei, LX; Xiue, S; Yan, MS, 1993
)
1.97

Effects

Norcantharidin (NCTD) has been used as a clinical antineoplastic drug in China for several years. diamminedichloroplatinum is a valuable clinical cancer chemotherapy agent.

ExcerptReferenceRelevance
"Norcantharidin (NCTD) has a certain degree of hydrophilicity and poor lipophilicity, and has some side-effects, including short t"( Preclinical evaluations of Norcantharidin liposome and emulsion hybrid delivery system with improved encapsulation efficiency and enhanced antitumor activity.
Dong, N; Gao, S; Gou, J; He, H; Liu, Z; Tan, X; Tang, X; Wu, Z; Yin, T; Zhang, Y; Zhao, L; Zhou, N, 2022
)
2.46
"Norcantharidin (NCTD) has a certain degree of hydrophilicity and poor lipophilicity, and has some side-effects, including short t"( Preclinical evaluations of Norcantharidin liposome and emulsion hybrid delivery system with improved encapsulation efficiency and enhanced antitumor activity.
Dong, N; Gao, S; Gou, J; He, H; Liu, Z; Tan, X; Tang, X; Wu, Z; Yin, T; Zhang, Y; Zhao, L; Zhou, N, 2022
)
2.46
"Norcantharidin (NCTD) has antiproliferation, antimetastasis, apoptosis, and autophagy effects in various tumor cells."( Norcantharidin combined with paclitaxel induces endoplasmic reticulum stress mediated apoptotic effect in prostate cancer cells by targeting SIRT7 expression.
Chen, YS; Chiou, HL; Hsieh, YH; Hui, SC; Lee, CH; Lin, CY; Wu, MH, 2021
)
2.79
"Norcantharidin (NCTD) has been used as a clinical antineoplastic drug in China for several years, and diamminedichloroplatinum is a valuable clinical cancer chemotherapy agent. "( Norcantharidin combined with diamminedichloroplatinum inhibits tumor growth and cancerometastasis of hepatic carcinoma in murine.
An, FY; Chen, XJ; Geng, GQ; Li, ZD; Liu, XS; Liu, YQ; Luo, LL; Sun, SB; Xie, XR; Zhang, XP, 2018
)
3.37
"Norcantharidin (NCTD) has shown to have multiple antitumor activities against GBCs, etc; however the exact mechanism is not thoroughly elucidated."( Norcantharidin inhibits tumor growth and vasculogenic mimicry of human gallbladder carcinomas by suppression of the PI3-K/MMPs/Ln-5γ2 signaling pathway.
Fan, YZ; Ge, CY; Liu, ZY; Lu, XS; Sun, W; Zhang, JT; Zhang, WZ; Zhao, ZM, 2014
)
2.57
"Norcantharidin has been used as an efficacious anticancer drug in China for many years, but its true mechanism remains poorly understood. "( Norcantharidin induces HT-29 colon cancer cell apoptosis through the alphavbeta6-extracellular signal-related kinase signaling pathway.
Agrez, M; Chen, R; Lin, P; Liu, E; Liu, X; Niu, J; Niu, W; Peng, C; Wang, J; Xu, K; Zhang, Z, 2009
)
3.24
"Norcantharidin not only has strong anticancer activity, but also eliminates most side-effects in the urinary system, does not cause myelosuppression and increases the number of white blood cells."( Norcantharidin analogues: a patent review (2006 - 2010).
Deng, L; Tang, S, 2011
)
2.53
"Norcantharidin (NCTD) has been reported to induce tumor cell apoptosis. "( Norcantharidin induces melanoma cell apoptosis through activation of TR3 dependent pathway.
Bing, Z; Bosenberg, M; Kumar, SM; Liu, S; Martin, JS; Sheng, W; Xu, X; Yu, H, 2011
)
3.25
"Norcantharidin (NCTD) has been reported to possess potent anti-angiogenesis and antitumor properties in several cell lines and xenograft tumor models."( Suppression of lymphangiogenesis in human lymphatic endothelial cells by simultaneously blocking VEGF-C and VEGF-D/VEGFR-3 with norcantharidin.
Fan, YZ; Jing, W; Liu, ZY; Ni, YY; Qiu, HO; Sun, JJ; Yuan, XJ, 2012
)
1.3

Actions

ExcerptReferenceRelevance
"Norcantharidin began to inhibit the invasion of GBC-SD cells at the concentration of 5 microg/mL, and the invasive action of GBC-SD cells was inhibited completely and their crossing-river time was prolonged significantly at 40 microg/mL."( Effect of norcantharidin on proliferation and invasion of human gallbladder carcinoma GBC-SD cells.
Chen, CQ; Fan, YZ; Fu, JY; Zhao, ZM, 2005
)
1.45

Treatment

Treatment by norcantharidin induced significant mitophagy and autophagy, as demonstrated by a decrease in Translocase Of Outer Mitochondrial Membrane 20 (TOM20), increased beclin1 and LC3-II protein expression, reduced protein SQSTM1/p62 expression, and accumulation of punctate LC3 in the cytoplasm of SK-N-SH cells. Treatment with norcanthan at 3mg/ml or higher significantly increased oligonucleosomal formation with concomitant appearance of PARP cleavage, implicating the induction of apoptosis.

ExcerptReferenceRelevance
"Norcantharidin-treated cells showed the activation of caspase 8."( Induction of apoptosis by norcantharidin in human colorectal carcinoma cell lines: involvement of the CD95 receptor/ligand.
Jiang, Y; Kan, B; Lei, S; Liu, JY; Lu, Y; Luo, F; Mao, YQ; Peng, F; Tian, L; Wang, GS; Wang, QR; Wei, YQ; Yang, L; Zhao, X; Zou, LQ, 2002
)
1.34
"Treatment by norcantharidin induced significant mitophagy and autophagy, as demonstrated by a decrease in Translocase Of Outer Mitochondrial Membrane 20 (TOM20), increased beclin1 and LC3-II protein expression, reduced protein SQSTM1/p62 expression, and accumulation of punctate LC3 in the cytoplasm of SK-N-SH cells."( Norcantharidin Inhibits SK-N-SH Neuroblastoma Cell Growth by Induction of Autophagy and Apoptosis.
Cao, M; Dai, L; Han, Z; Jiang, J; Li, B; Li, Z; Wang, J; Zhang, X, 2017
)
2.25
"Treatment with norcantharidin at 3μg/ml or higher significantly increased oligonucleosomal formation with concomitant appearance of PARP cleavage, implicating the induction of apoptosis."( Norcantharidin induces apoptosis in human prostate cancer cells through both intrinsic and extrinsic pathways.
Chou, CY; Hu, DN; Kao, YH; Lin, IC; Wu, YC; Yang, PY, 2016
)
2.22
"Treatment of norcantharidin with allylamine afforded the corresponding allyl-norcantharimide (20) which was amenable to epoxidation (mCPBA, 22) and subsequent ring opening (MeOH/H(+); 23) or alternatively, osmylation (OsO(4)/NMO; 24)."( Norcantharimides, synthesis and anticancer activity: Synthesis of new norcantharidin analogues and their anticancer evaluation.
Ackland, SP; Gilbert, J; Hill, TA; McCluskey, A; Sakoff, JA; Sauer, B; Stewart, SG, 2007
)
0.93
"Treatment with norcantharidin of colorectal cancer cells not only inhibited cell proliferation, but also induced apoptosis. "( Induction of apoptosis by norcantharidin in human colorectal carcinoma cell lines: involvement of the CD95 receptor/ligand.
Jiang, Y; Kan, B; Lei, S; Liu, JY; Lu, Y; Luo, F; Mao, YQ; Peng, F; Tian, L; Wang, GS; Wang, QR; Wei, YQ; Yang, L; Zhao, X; Zou, LQ, 2002
)
0.97

Toxicity

ExcerptReferenceRelevance
"The norcantharidin/poloxamer 407 is less toxic than the equivalent dose of norcantharidin, mainly because norcantharidin/poloxamer 407 may release norcantharidin sustainedly, thus reducing norcantharidin concentration in blood."( [Comparison of acute toxicity of two preparations of norcantharidin in mice].
Gu, W; Li, B; Zhang, YN; Zhu, LF, 2007
)
1.15
" However, the clinical use of NCTD is limited due to its poor solubility, low bioavailability, and toxic effects on normal cells."( Strategies for Solubility and Bioavailability Enhancement and Toxicity Reduction of Norcantharidin.
Li, X; Liu, Q; Sheng, H; Sun, H; Zhu, L, 2022
)
0.95

Pharmacokinetics

ExcerptReferenceRelevance
" The method was suitable for determination of low NCTD concentration in human serum after therapeutic oral doses, and has been successfully used for pharmacokinetic studies in healthy Chinese volunteers."( Determination and pharmacokinetic study of norcantharidin in human serum by HPLC-MS/MS method.
Guo, RC; Wang, BJ; Wei, CM; Yuan, GY; Zhang, R, 2008
)
0.61
" Pharmacokinetic profiles of the NCTD group and PVP-NCTD-NP group, after oral and intravenous administration in rats, revealed that relative bioavailabilities were 173."( Pharmacokinetics, tissue distribution, and metabolites of a polyvinylpyrrolidone-coated norcantharidin chitosan nanoparticle formulation in rats and mice, using LC-MS/MS.
Chen, WL; Ding, XY; Gu, ZL; Hong, CJ; Liu, Y; Shi, LS; Xing, KL; Zhang, Q; Zhang, XN; Zhu, AJ, 2012
)
0.6
" However, the unreliable pharmacokinetic characteristics of DM-NCTD could result in low bioavailability, hindering the clinical use of DM-NCTD in the treatment of diseases."( Liquid chromatography-tandem mass spectrometry evaluation of the pharmacokinetics of a diacid metabolite of norcantharidin loaded in folic acid-targeted liposomes in mice.
Gao, JQ; Han, M; Liu, MC; Ma, XQ; Peng, LH; Xu, Y, 2016
)
0.65

Compound-Compound Interactions

ExcerptReferenceRelevance
" Cell cycle and cell apoptosis were assessed by flow cytometry (FCM) combined with PI staining and annexin V-FITC/PI, respectively."( [Inhibitory effect of norcantharidin combined with evodiamine on the growth of human hepatic carcinoma cell line HepG2 in vitro].
Liao, H; Liu, Y; You, Z; Zahng, J, 2014
)
0.72
"EVO combined with NCTD showed synergetic effect on anti-proliferation and pro-apoptosis in HepG2 cells."( [Inhibitory effect of norcantharidin combined with evodiamine on the growth of human hepatic carcinoma cell line HepG2 in vitro].
Liao, H; Liu, Y; You, Z; Zahng, J, 2014
)
0.72
"To study the therapeutic effect of norcantharidin (NCTD) combined with ABT-737 on hepatocellular carcinoma cells and the molecular mechanism."( Norcantharidin combined with ABT-737 for hepatocellular carcinoma: Therapeutic effects and molecular mechanisms.
Li, G; Lin, L; Ren, J; Ye, T; Zhao, W, 2016
)
2.15
" Liver cancer cells in the logarithmic phase of growth were vaccinated and cultured to the cell wall stage; these cells were treated for 48 h with different concentrations of NCTD, or ABT-737, or NCTD combined with ABT-737."( Norcantharidin combined with ABT-737 for hepatocellular carcinoma: Therapeutic effects and molecular mechanisms.
Li, G; Lin, L; Ren, J; Ye, T; Zhao, W, 2016
)
1.88
"As the concentration of NCTD increased, the cell proliferation inhibition rate gradually decreased; and the treatment effect of ABT-737 1-3 μm combined with NCTD on cell proliferation inhibition was stronger than that of ABT-737 alone."( Norcantharidin combined with ABT-737 for hepatocellular carcinoma: Therapeutic effects and molecular mechanisms.
Li, G; Lin, L; Ren, J; Ye, T; Zhao, W, 2016
)
1.88
"NCTD combined with ABT-737 has a positive role in the treatment of HCC, and it has great value in clinical research."( Norcantharidin combined with ABT-737 for hepatocellular carcinoma: Therapeutic effects and molecular mechanisms.
Li, G; Lin, L; Ren, J; Ye, T; Zhao, W, 2016
)
1.88
" Nevertheless, the antitumor effect of NCTD combined with paclitaxel (PTX), a chemotherapeutic drug, in PCa remains unknown."( Norcantharidin combined with paclitaxel induces endoplasmic reticulum stress mediated apoptotic effect in prostate cancer cells by targeting SIRT7 expression.
Chen, YS; Chiou, HL; Hsieh, YH; Hui, SC; Lee, CH; Lin, CY; Wu, MH, 2021
)
2.06

Bioavailability

ExcerptReferenceRelevance
" The absorption rate constants (Ka) of NCTD at different segments were found to be duodenum > jejunum > ileum > colon."( Novel norcantharidin-loaded liver targeting chitosan nanoparticles to enhance intestinal absorption.
Bei, YY; Chen, WL; Chen, XY; Gu, ZL; Liu, Y; Shi, LS; Wang, Q; Wang, WJ; Xing, KL; Xu, JY; Zhang, Q; Zhang, XN; Zhu, AJ, 2012
)
0.86
" A liposomal drug delivery system could overcome the shortcomings of DM-NCTD by improving the relative bioavailability (Fr), reducing drug toxicity, and increasing the therapeutic efficacy."( Liquid chromatography-tandem mass spectrometry evaluation of the pharmacokinetics of a diacid metabolite of norcantharidin loaded in folic acid-targeted liposomes in mice.
Gao, JQ; Han, M; Liu, MC; Ma, XQ; Peng, LH; Xu, Y, 2016
)
0.65
" This review summarizes the structure-activity relationship of NCTD and novel strategies to improve the solubility and bioavailability of NCTD as well as reduce the toxicity."( Strategies for Solubility and Bioavailability Enhancement and Toxicity Reduction of Norcantharidin.
Li, X; Liu, Q; Sheng, H; Sun, H; Zhu, L, 2022
)
0.95
" Therefore, this review focused on the studies of targeted drug delivery systems combined with NCTD in recent years, including passive and active targeted drug delivery systems, and physicochemical targeted drug delivery systems for improving drug bioavailability and enhancing its efficacy, as well as increasing drug targeting ability and reducing its adverse effects."( Review targeted drug delivery systems for norcantharidin in cancer therapy.
Cheng, JX; Fan, Y; Guo, DY; Shi, YJ; Sun, J; Tian, H; Zhai, BT; Zhang, XF; Zou, JB, 2022
)
0.99

Dosage Studied

ExcerptRelevanceReference
" DM-NCTD had dose-dependent kinetics across the dosage range investigated, with enhanced T(1/2α) and AUC(0-12) and apparently decreasing V(d) and CL with increasing dosage."( Determination and pharmacokinetic study of the diacid metabolite of norcantharidin in beagle plasma by use of liquid chromatography-tandem mass spectrometry.
Guo, M; Jin, Z; Li, F; Li, W; Liu, M; Ma, X, 2013
)
0.63
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
furofuranOrganic heterobicyclic compounds containing a two furan rings ortho-fused to each other.
[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 Targets (16)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency22.98330.004023.8416100.0000AID485290
Chain A, Beta-lactamaseEscherichia coli K-12Potency5.62340.044717.8581100.0000AID485294
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency29.83040.177814.390939.8107AID2147
ATAD5 protein, partialHomo sapiens (human)Potency15.62670.004110.890331.5287AID493106; AID504466; AID504467
GLS proteinHomo sapiens (human)Potency3.54810.35487.935539.8107AID624146
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency26.60320.001530.607315,848.9004AID1224821
arylsulfatase AHomo sapiens (human)Potency0.84921.069113.955137.9330AID720538
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency37.68580.035520.977089.1251AID504332
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency75.686323.934123.934123.9341AID1967
ras-related protein Rab-9AHomo sapiens (human)Potency125.89200.00022.621531.4954AID485297
gemininHomo sapiens (human)Potency11.22020.004611.374133.4983AID463097
DNA polymerase kappa isoform 1Homo sapiens (human)Potency0.39810.031622.3146100.0000AID588579
lamin isoform A-delta10Homo sapiens (human)Potency17.72010.891312.067628.1838AID1459; AID1487
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency28.18381.000010.475628.1838AID1457
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
PPP5C protein, partialHomo sapiens (human)IC50 (µMol)2.56700.82781.69742.5670AID2422
serine/threonine-protein phosphatase PP1-alpha catalytic subunit isoform 3Homo sapiens (human)IC50 (µMol)2.83202.47703.65556.6460AID2403
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (22)

Assay IDTitleYearJournalArticle
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings 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.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS 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.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1159550Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening2015Nature cell biology, Nov, Volume: 17, Issue:11
6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (268)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901 (0.37)18.7374
1990's10 (3.73)18.2507
2000's53 (19.78)29.6817
2010's161 (60.07)24.3611
2020's43 (16.04)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 26.07

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 moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index26.07 (24.57)
Research Supply Index5.61 (2.92)
Research Growth Index5.88 (4.65)
Search Engine Demand Index31.58 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (26.07)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews8 (2.94%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other264 (97.06%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (1)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Phase I Clinical Study for Evaluation of Pharmacokinetic, Safety, Tolerance of Norcantharidin Lipid Microsphere for Injection in Patients With Solid Tumor [NCT04673396]Phase 136 participants (Anticipated)Interventional2020-09-22Recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]