Page last updated: 2024-12-07

mizoribine

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Mizoribine is an immunosuppressant drug used in the treatment of organ transplantation rejection and autoimmune diseases. It is a purine analog that inhibits the synthesis of DNA and RNA, thereby blocking the proliferation of lymphocytes, the cells responsible for immune responses. Its synthesis involves a series of chemical reactions, starting with the conversion of guanine to 6-thioguanine followed by a series of modifications to yield the final product. Mizoribine has been shown to be effective in preventing organ rejection and has also been used to treat autoimmune diseases such as rheumatoid arthritis and systemic lupus erythematosus. The drug's importance stems from its ability to suppress the immune system, which is crucial for preventing organ rejection and managing autoimmune diseases. Mizoribine is studied to understand its mechanism of action, optimize its therapeutic use, and develop novel immunosuppressant drugs with improved efficacy and fewer side effects.'

Cross-References

ID SourceID
PubMed CID104762
CHEMBL ID245019
CHEBI ID31858
SCHEMBL ID7118
MeSH IDM0055297

Synonyms (117)

Synonym
AC-5266
MLS001076272
1-((2r,3r,4s,5r)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-5-hydroxy-1h-imidazole-4-carboxamide
50924-49-7
1-[(2r,3r,4s,5r)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl]-5-hydroxy-imidazole-4-carboxamide
5-hydroxy-1-beta-d-ribofuranosyl-1h-imidazole-4-carboxamide
mizoribine ,
DIVK1C_000948
KBIO1_000948
smr000058473
he-69
MLS000028813 ,
brn 4151713
anhydro-4-carbamoyl-5-hydroxy-1-beta-d-ribofuranosyl-imidazolium hydroxide
mizoribine [inn:jan]
5-hydroxy-1-beta-d-ribofuranosylimidazole-4-carboxamide
1h-imidazole-4-carboxamide, 5-hydroxy-1-beta-d-ribofuranosyl-
mizoribinum [inn-latin]
mizoribina [inn-spanish]
4-carbamoyl-1-beta-d-ribofuranosyl-imidazolium-5-olate
bredinine
EU-0100745
mizoribine, >=98% (tlc)
BSPBIO_002298
SMP1_000195
1h-imidazole-4-carboxamide, 5-hydroxy-1-.beta.-d-ribofuranosyl-
nsc-289637
bredinin
IDI1_000948
SPECTRUM5_001671
D01392
bredinin (tn)
mizoribine (jp17/inn)
KBIOGR_000859
KBIO3_001518
SPBIO_001438
SPECTRUM4_000220
SPECTRUM3_000739
NINDS_000948
SPECTRUM2_001559
LOPAC0_000745
NCGC00094087-02
NCGC00094087-01
NCGC00094087-03
M 3047 ,
n'-(beta-d-ribofuranosyl)-5-hydroxyimidazole-4-carboxamide
NCGC00094087-04
CHEMBL245019
HMS502P10
he 69
1-[(2r,3r,4s,5r)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-hydroxyimidazole-4-carboxamide
HMS3262E12
dtxcid6025777
dtxsid8045777 ,
tox21_111242
cas-50924-49-7
HMS2230D04
AKOS015994615
CCG-39778
BCP9000933
mizoribina
mizoribinum
nsc 289637
unii-4jr41a10vp
4jr41a10vp ,
mizoribine(bredinin)
BCP0726000318
mizoribine hydrobromide
LP00745
S1384
mizoribine [mi]
mizoribine [jan]
mizoribine [mart.]
mizoribine [inn]
mizoribine [who-dd]
5-hydroxy-1-.beta.-d-ribofuranosylimidazole-4-carboxamide
CS-1823
HY-17470
MLS006010038
SCHEMBL7118
NCGC00094087-05
tox21_111242_1
HS-0046 ,
J-700185
NCGC00261430-01
tox21_500745
HZQDCMWJEBCWBR-UUOKFMHZSA-N
50524-49-7
cid_104762
bdbm68669
1-[(2r,3r,4s,5r)-3,4-dihydroxy-5-(hydroxymethyl)-2-oxolanyl]-5-hydroxy-4-imidazolecarboxamide
1-[(2r,3r,4s,5r)-3,4-dihydroxy-5-methylol-tetrahydrofuran-2-yl]-5-hydroxy-imidazole-4-carboxamide
1-[(2r,3r,4s,5r)-5-(hydroxymethyl)-3,4-bis(oxidanyl)oxolan-2-yl]-5-oxidanyl-imidazole-4-carboxamide
1-(beta-d-ribofuranosyl)-5-hydroxyimidazole-4-carboxamide
M2399
AB00053323_12
AB00053323_13
OPERA_ID_1558
mfcd00057221
5-hydroxy-1-b-d-ribofuranosyl-1h-imidazole-4-carboxamide
1-[(2r,3r,4s,5r)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-hydroxy-1h-imidazole-4-carboxamide
SR-01000075989-1
sr-01000075989
CHEBI:31858
SR-01000075989-4
SBI-0050723.P003
DB12617
mizoribine (bredinin)
EX-A2256
Q6884708
A16794
SDCCGSBI-0050723.P004
1h-imidazole-4-carboxamide, 5-hydroxy-1-b-d-ribofuranosyl-
nsc 289637;he 69
50924-49-7 (non-salt)
FD9057
BP-58612

Research Excerpts

Overview

Mizoribine (MZR) is an oral immunosuppressant that inhibits inosine monophosphate dehydrogenase. It is widely used in Japan for the treatment of autoimmune diseases and nephrotic syndrome, as well as after renal transplantation.

ExcerptReferenceRelevance
"Mizoribine is an oral immunosuppressant that inhibits inosine monophosphate dehydrogenase and is widely used in Japan for the treatment of autoimmune diseases and nephrotic syndrome, as well as after renal transplantation."( Fanconi syndrome in an elderly patient with membranous nephropathy during treatment with the immunosuppressant mizoribine.
Fukushima, S; Iwano, M; Kasuno, K; Kimura, H; Kobayashi, M; Mikami, D; Morita, S; Naiki, H; Nishikawa, S; Nishikawa, Y; Nishimori, K; Sakashita, S; Shimamoto, Y; Takahashi, N; Yokoi, S, 2023
)
1.84
"Mizoribine (MZR) is an emerging treatment option for nephrotic syndrome; however, its dosage and administration are yet lack of consensus."( Effect of mizoribine pulse therapy in adult membranous nephropathy.
Chang, W; Han, Y; Liu, Y; Wang, X; Zhang, M; Zhang, W, 2021
)
1.75
"Mizoribine is an immunosuppressive drug with fewer side effects than prednisolone."( Study protocol: high-dose mizoribine with prednisolone therapy in short-term relapsing steroid-sensitive nephrotic syndrome to prevent frequent relapse (JSKDC05 trial).
Hama, T; Iijima, K; Ishikura, K; Ito, S; Nakamura, H; Nakanishi, K; Nozu, K; Saito-Oba, M; Sako, M; Shima, Y; Yoshikawa, N, 2018
)
1.5
"Mizoribine (MZR) is an immunosuppressant used to treat adult nephropathy. "( Usefulness of mizoribine administration in children with frequently relapsing nephrotic syndrome, and the relationship between pharmacokinetic parameters and efficacy: a multicenter prospective cohort study in China.
Dang, XQ; Gao, YF; Jiang, XY; Rong, LP; Shen, Q; Xia, ZK; Xu, H; Yi, ZW, 2019
)
2.32
"Mizoribine (MZR) is a selective inhibitor of the inosine monophosphate dehydrogenase - a key enzyme in the de novo pathway of guanine nucleotides - that was developed in Japan. "( Mizoribine selectively attenuates monocyte chemoattractant protein-1 production in cultured human glomerular mesangial cell: a possible benefit of its use in the treatment of lupus nephritis.
Aizawa, T; Chiba, Y; Imaizumi, T; Matsumiya, T; Tanaka, H; Tsuruga, K; Watanabe, S; Yoshida, H, 2014
)
3.29
"Mizoribine (MZR) is a selective inhibitor of inosine monophosphate dehydrogenase, a key enzyme in the pathway responsible for de novo synthesis of guanine nucleotides. "( Mizoribine in the treatment of pediatric-onset glomerular disease.
Imaizumi, T; Tanaka, H; Tsuruga, K, 2015
)
3.3
"Mizoribine is an imidazole nucleoside and a novel immunosuppressant that has been used to treat other immune-related diseases."( Treatment of membranous nephropathy with mizoribine: A control trial.
An, W; Liu, Y; Song, X; Tu, Y; Wang, X; Zhang, W, 2016
)
1.42
"Mizoribine (MZR) is an immunosuppressive agent that exhibits a less potent immunosuppressive effect at doses up to 3 mg/kg/d. "( Efficacy and Safety of High-Dose Mizoribine Combined With Cyclosporine, Basiliximab, and Corticosteroids in Renal Transplantation: A Japanese Multicenter Study.
Akioka, K; Fujisawa, M; Fukuda, Y; Horimi, T; Ito, SI; Nakatani, T; Nishimura, K; Sugitani, A; Uchida, K; Ushigome, H; Yoshimura, N; Yuzawa, K, 2016
)
2.16
"Mizoribine (MZB) is a newly developed immunosuppressive drug with few adverse effects; however, there are currently few studies using MZB in adult patients with IgAV."( Efficacy of mizoribine and prednisolone combination therapy in adult patients with IgA vasculitis.
Mima, A, 2017
)
1.56
"Mizoribine is a purine antimetabolite that inhibits T cell activation/proliferation and B cell proliferation."( Successful treatment of refractory polymyositis with the immunosuppressant mizoribine: case report.
Hirakata, M; Kaneko, Y; Kuwana, M; Sato, S; Suwa, A; Suzuki, Y, 2009
)
1.3
"Mizoribine is a disease-modifying anti-rheumatic drug (DMARD) that is used in the treatment of rheumatoid arthritis. "( Mizoribine may suppress bone erosion in patients with rheumatoid arthritis by inhibiting osteoclastogenesis.
Bang, JS; Choi, HM; Hong, SJ; Jo, YJ; Kim, KS; Lee, SH; Lee, YA; Oh, DH; Park, EK; Yang, HI; Yoo, MC, 2009
)
3.24
"Mizoribine (MZB) is an imidazole nucleoside and an immunosuppressive agent. "( Mizoribine: a new approach in the treatment of renal disease.
Kawasaki, Y, 2009
)
3.24
"Mizoribine (MZR) is an imidazole nucleoside used as a therapeutic immunosuppressive agent. "( The immunosuppressive drug mizoribine directly prevents podocyte injury in puromycin aminonucleoside nephrosis.
Hiromura, K; Kaneko, Y; Kuroiwa, T; Maeshima, A; Nojima, Y; Sakairi, T; Takahashi, S; Takeuchi, S; Tomioka, M, 2010
)
2.1
"Mizoribine (MZ) is a potent immunosuppressant used in conjunction with other immunosuppressants to prevent and treat allograft rejection after organ transplantation. "( Acute allograft renal failure with marked hyperuricemia developing during mizoribine administration: a case report with review of the literature.
Guo, HB, 2010
)
2.03
"Mizoribine (MZR) is an immunosuppressant that inhibits nucleic acid metabolism and is a relatively safe disease-modifying anti-rheumatic drug (DMARD). "( Efficacy and safety of mizoribine by one single dose administration for patients with rheumatoid arthritis.
Aramaki, T; Arima, K; Eguchi, K; Fujikawa, K; Ichinose, K; Ida, H; Iwamoto, N; Kamachi, M; Kawakami, A; Kawashiri, SY; Nakamura, H; Origuchi, T; Tamai, M; Tsukada, T; Ueki, Y, 2010
)
2.11
"Mizoribine (MZR) is an inosine monophosphate dehydrogenase inhibitor. "( Mizoribine--an inosine monophosphate dehydrogenase inhibitor--acts synergistically with cyclosporine A in prolonging survival of murine islet cell and heart transplants across major histocompatibility barrier.
Angaswamy, N; Fukami, N; Hoshinaga, K; Liu, W; Mohanakumar, T; Subramanian, V, 2012
)
3.26
"Mizoribine (MZR) is an immunosuppressive drug and it has been used for organ transplantation and treatment of various autoimmune diseases."( Mizoribine suppresses proliferation of rat glomerular epithelial cells in culture and inhibits increase of monocyte chemoattractant protein-1 and macrophage inflammatory protein-2 stimulated by thrombin.
Fujita, T; Murakami, R; Nakamura, N; Shimada, M; Shimaya, Y; Yamabe, H, 2012
)
2.54
"Mizoribine is a newly developed immunosuppressive agent that has low toxicity."( Mizoribine treatment for antihistamine-resistant chronic autoimmune urticaria.
Dainichi, T; Hamada, T; Hashimoto, T; Hide, M; Ishii, K; Ishii, N; Karashima, T; Kawakami, T; Nakama, T; Tsuruta, D,
)
2.3
"Mizoribine (MZR) is an immunosuppressive agent and is used against RA in the same manner as methotrexate and tacrolimus."( Chronopharmacology of mizoribine in collagen-induced arthritis rats.
Kanasaki, Y; Sasaki, H; To, H; Tomonari, M, 2012
)
1.41
"Mizoribine (MZR) is an immunosuppressant used for the treatment of glomerular diseases, but there are few reports on the pharmacokinetics of MZR in children."( Mizoribine requires individual dosing due to variation of bioavailability.
Abe, Y; Fuke, T; Hibino, S; Itabashi, K; Murayama, J; Nakano, Y; Saito, T; Sakurai, S; Takeshi, M; Watanabe, S, 2012
)
3.26
"Mizoribine (MZR) is a newly developed immunosuppressive agent in Japan. "( Mizoribine oral pulse therapy for patients with disease flare of lupus nephritis.
Ito, E; Nakahata, T; Suzuki, K; Tanaka, H; Tsugawa, K; Waga, S, 2003
)
3.2
"Mizoribine (MZR) is a novel immunosuppressant developed in Japan. "( Efficacy of mizoribine in the treatment of systemic lupus erythematosus in children.
Imanaka, H; Kawano, Y; Maeno, N; Ohkawa, T; Takei, S; Yoshidome, K, 2004
)
2.15
"Mizoribine (MZR) is a novel selective inhibitor of inosine monophosphatase dehydrogenase that was developed in Japan. "( Implication of the peak serum level of mizoribine for control of the serum anti-dsDNA antibody titer in patients with lupus nephritis.
Ito, E; Kudo, M; Nakahata, T; Suzuki, K; Tanaka, H; Tsugawa, K, 2005
)
2.04
"Mizoribine (MZR) is a purine antimetabolic immunosuppressant agent that has few little severe adverse events. "( Effects of long-term treatment with mizoribine in patients with proliferative lupus nephritis.
Koike, M; Moriyama, T; Naito, M; Nihei, H; Nitta, K; Otsubo, S; Suganuma, S; Takei, T; Uchida, K; Yumura, W, 2005
)
2.05
"Mizoribine is an immunosuppressive agent that was developed in Japan and has been found to inhibit the proliferation of lymphocytes, especially B cells."( Combination therapy of prednisolone and mizoribine improves cryoglobulinemic vasculitis with purpura and skin ulcers.
Hamaguchi, M; Ishino, H; Kawahito, Y; Kohno, M; Tsubouchi, Y; Wada, M; Yamamoto, A; Yoshikawa, T, 2007
)
1.33
"Mizoribine (MZR) is a novel purine synthesis inhibitor that was developed in Japan. "( Long-term mizoribine intermittent pulse therapy for young patients with flare of lupus nephritis.
Ito, E; Nakahata, T; Suzuki, K; Tanaka, H; Tsugawa, K, 2006
)
2.18
"Mizoribine is an oral immunosuppressive agent approved in several countries for prevention of rejection in renal transplantation. "( Safety, tolerability and pharmacokinetics of higher-dose mizoribine in healthy male volunteers.
Combs, M; Ishikawa, H; Obaidi, M; Stewart, AJ; Stypinski, D; Weber, M, 2007
)
2.03
"Mizoribine is an amphoteric compound, however, the suppression of intestinal absorption by bile salts was not ascribed to the electrostatic interaction or micellar formation between mizoribine and bile salts."( Characterization of intestinal absorption of mizoribine mediated by concentrative nucleoside transporters in rats.
Kamio, Y; Mori, N; Murakami, T; Yokooji, T, 2008
)
1.33
"Mizoribine (MIZ) is a novel imidazole nucleoside with immunosuppressive activity. "( Functional interaction of the immunosuppressant mizoribine with the 14-3-3 protein.
Gustafsson, JA; Itoh, H; Takahashi, S; Wakui, H; Zilliacus, J, 2000
)
2.01
"Mizoribine is a new immunosuppressive drug and was authorized by the Japanese Government in 1984. "( Mizoribine: mode of action and effects in clinical use.
Yokota, S, 2002
)
3.2
"Mizoribine is a relatively safe and effective immunosuppressant."( Nephrotic syndrome and mizoribine in children.
Honda, M, 2002
)
1.35
"Mizoribine is an effective immunosuppressive drug in human renal transplantation."( Role of mizoribine in renal transplantation.
Tsuzuki, K, 2002
)
1.47
"Mizoribine (Mz) is an analogue of azathioprine (Az) with less hepatotoxicity, being extensively used as immunosuppressant in place of the latter agent especially in Japan. "( Advantages of triple therapy with mizoribine, cyclosporine and prednisolone over other types of triple and/or double therapy including cyclosporine for renal transplantation.
Bekku, Y; Inoue, S; Ishida, Y; Mita, K; Nagao, T; Nishimura, Y; Sugimoto, H; Tomikawa, S; Uchida, H; Watanabe, K, 1991
)
2

Effects

Mizoribine (MZR) has a less potent immunosuppressive effect up to 3 mg/kg/day MZR. It selectively inhibits the proliferation of lymphocytes by interfering with inosine monophosphate dehydrogenase. MizOribine has been successfully used without serious adverse effects in patients with various types of glomerulonephritis.

ExcerptReferenceRelevance
"Mizoribine (MZ) has been developed as an immunosuppressive agent in Japan, but it has a less-potent immunosuppressive effect up to 3 mg/kg/d. "( Beneficial Effects of High-Dose Mizoribine on ABO-Incompatible Living-Related Kidney Transplantation: Two-Year Results by a Japanese Multicenter Study.
Akioka, K; Akutsu, N; Harada, S; Nakamura, T; Nakatani, T; Ushigome, H; Yoshimura, N, 2017
)
2.18
"Mizoribine (MZR) has been developed as an immunosuppressant and is widely used in Asia. "( Long-term Survival Analysis of Kidney Transplant Recipients Receiving Mizoribine as a Maintenance Immunosuppressant: A Single-Center Study.
Kim, HY; Kim, JK; Lee, D; Lee, JH; Oh, JS; Sin, YH, 2019
)
2.19
"Mizoribine (MZR) has been developed as an immunosuppressive agent in Japan, but has a less potent immunosuppressive effect up to 3 mg/kg/d. "( Usefulness and safety of high-dose mizoribine on ABO-incompatible living related kidney transplantation using anti-CD20 and anti-CD25 antibodies without splenectomy: 3-year results.
Harada, S; Ito, T; Koshino, K; Nakamura, T; Nakao, T; Nobori, S; Sakai, K; Suzuki, T; Ushigome, H; Yoshimura, N, 2014
)
2.12
"Mizoribine has been recognized to have an acceptable toxicity profile compared with other immunosuppressants. "( A sudden onset of diabetic ketoacidosis and acute pancreatitis after introduction of mizoribine therapy in a patient with rheumatoid arthritis.
Ebihara, K; Mori, S, 2008
)
2.01
"Mizoribine (MZR) has been successfully used without serious adverse effects in patients with various types of glomerulonephritis, but there are only a few pharmacokinetic studies of MZR. "( Pharmacokinetic study of mizoribine in child-onset glomerulonephritis.
Abe, Y; Fuke, T; Hisano, M; Itabashi, K; Mikawa, T; Tsuji, Y; Watanabe, S, 2008
)
2.09
"Mizoribine (MZR) has shown to be effective against antineutrophil cytoplasmic antibody (ANCA)-related vasculitis; however, no reports have described the successful treatment of steroid-resistant ANCA-related vasculitis with MZR in patients with renal insufficiency requiring hemodialysis. "( A case report of steroid-resistant antineutrophil cytoplasmic antibody-related vasculitis successfully treated by mizoribine in a hemodialysis patient.
Abe, H; Fujimatsu, S; Furuno, Y; Kabashima, N; Matsumoto, M; Miyamoto, T; Miyazaki, M; Muta, T; Okazaki, M; Otsuji, Y; Serino, R; Shibata, T; Takeuchi, M; Tamura, M; Tokunaga, M, 2009
)
2.01
"Mizoribine (MZR) has been developed as an immunosuppressive agent in Japan, but it shows less potent immunosuppressive effects at doses up to 3 mg/kg/d. "( The efficacy and safety of high-dose mizoribine in ABO-incompatible kidney transplantation using anti-CD20 and anti-CD25 antibody without splenectomy treatment.
Matsuyama, M; Nobori, S; Okajima, H; Okamoto, M; Sakai, K; Suzuki, T; Ushigome, H; Yoshimura, N, 2012
)
2.09
"Mizoribine (MZR) has been developed as an immunosuppressive agent, but has a less potent immunosuppressive effect up to 3 mg/kg/day MZR. "( The beneficial effect of high-dose mizoribine combined with cyclosporine, basiliximab, and corticosteroids on CMV infection in renal transplant recipients.
Akioka, K; Nobori, S; Okamoto, M; Sakai, K; Suzuki, T; Ushigome, H; Yoshimura, N, 2013
)
2.11
"Mizoribine (MZR) has been shown to possess immunosuppressive activity that selectively inhibits the proliferation of lymphocytes by interfering with inosine monophosphate dehydrogenase. "( Effects of mizoribine on MHC-restricted exogenous antigen presentation in dendritic cells.
Ha, NJ; Han, S; Kim, H; Kim, K; Kwon, J; Lee, CK; Lee, SJ; Lee, YH; Song, Y, 2006
)
2.17
"Mizoribine has been used to prevent rejection of organ allografts in humans and in animal models. "( Inhibition of expression of cyclin A in human B cells by an immunosuppressant mizoribine.
Hirohata, S; Yanagida, T, 1995
)
1.96
"Mizoribine has been shown to have beneficial effects in the treatment of rheumatoid arthritis and lupus nephritis, in which abnormal B cell functions are involved. "( Inhibition of cyclin A gene expression in human B cells by an immunosuppressant mizoribine.
Hirohata, S; Nakanishi, K; Yanagida, T, 2000
)
1.98
"Mizoribine has been shown to possess an immunosuppressive action that inhibits the proliferation of lymphocytes selectively by interfering with inosine monophosphate dehydrogenase. "( Mizoribine ameliorates the tubulointerstitial fibrosis of obstructive nephropathy.
Kai, K; Kobayashi, Y; Mitarai, T; Ogawa, S; Sato, N; Shiraiwa, K; Utsunomiya, Y; Watanabe, A; Yamagishi-Imai, H, 2001
)
3.2
"Mizoribine has been reported as an effective and safe drug for patients with FRNS. "( Nephrotic syndrome and mizoribine in children.
Honda, M, 2002
)
2.07

Actions

Mizoribine (MZR) can inhibit mesangial cell (MC) proliferation, but the mechanism remains unknown. Mizoribin was found to inhibit in vitro osteoclastogenesis in a dose-dependent manner.

ExcerptReferenceRelevance
"Mizoribine was found to inhibit in vitro osteoclastogenesis in a dose-dependent manner."( Mizoribine may suppress bone erosion in patients with rheumatoid arthritis by inhibiting osteoclastogenesis.
Bang, JS; Choi, HM; Hong, SJ; Jo, YJ; Kim, KS; Lee, SH; Lee, YA; Oh, DH; Park, EK; Yang, HI; Yoo, MC, 2009
)
2.52
"Mizoribine (MZR) can inhibit mesangial cell (MC) proliferation, but the mechanism remains unknown. "( A novel target of mizoribine inhibiting mesangial cell proliferation: S phase kinase-associated protein 2.
Chang, M; Chen, X; Fu, B; Hong, Q; Liu, S; Lv, Y; Qin, F; Shi, S; Wang, J; Xie, Y; Yin, Z; Zhang, X, 2010
)
2.14

Treatment

Treatment with mizoribine reduced intracellular GTP levels and induced morphologic and functional differentiation in these two cell lines. Treatment ameliorated the increase in interstitial volume induced by UUO.

ExcerptReferenceRelevance
"Treatment with mizoribine reduced intracellular GTP levels and induced morphologic and functional differentiation in these two cell lines in a dose-dependent manner."( Differentiation induction in non-lymphocytic leukemia cells upon treatment with mizoribine.
Huberman, E; Inai, K; Nakamura, T; Tsutani, H; Ueda, T; Yamauchi, T, 1997
)
0.86
"Treatment with mizoribine ameliorated the increase in interstitial volume induced by UUO."( Mizoribine ameliorates the tubulointerstitial fibrosis of obstructive nephropathy.
Kai, K; Kobayashi, Y; Mitarai, T; Ogawa, S; Sato, N; Shiraiwa, K; Utsunomiya, Y; Watanabe, A; Yamagishi-Imai, H, 2001
)
2.09

Toxicity

Mizoribine (MZR) is an immunosuppressant that inhibits nucleic acid metabolism and is a relatively safe disease-modifying anti-rheumatic drug (DMARD) We investigated whether high-dose Mizoribin, 4-6 mg/kg/d was as effective and safe as mycophenolate mofetil (MMF) for patients after kidney transplantation.

ExcerptReferenceRelevance
" Our data also suggest that the drugs may reduce mutant HPRT-deficient somatic cells in vivo, and may cause enhanced adverse reactions in HPRT-deficient individuals."( Differential cytotoxic effects of mizoribine and its aglycone on human and murine cells and on normal and enzyme-deficient human cells.
Hakoda, M; Kamatani, N; Kashiwazaki, S; Terai, C; Yamanaka, H, 1995
)
0.57
" It had minimum adverse effects, however, MZR therapy does not sufficiently suppress the relapse of FRNS."( [Beneficial and adverse effects of high-dosage MZR therapy in the management of children with frequently relapsing nephrotic syndrome].
Goto, M; Hamasaki, Y; Hataya, H; Honda, M; Ikeda, M; Ishikura, K, 2006
)
0.33
" No other adverse effect was observed."( [Beneficial and adverse effects of high-dosage MZR therapy in the management of children with frequently relapsing nephrotic syndrome].
Goto, M; Hamasaki, Y; Hataya, H; Honda, M; Ikeda, M; Ishikura, K, 2006
)
0.33
"High-dose MZR therapy in the management for FRNS may provide more beneficial effects without significant adverse effects."( [Beneficial and adverse effects of high-dosage MZR therapy in the management of children with frequently relapsing nephrotic syndrome].
Goto, M; Hamasaki, Y; Hataya, H; Honda, M; Ikeda, M; Ishikura, K, 2006
)
0.33
"We investigated whether high-dose Mizoribine (MIZ: a water-soluble anti-metabolite), 4-6 mg/kg/d was as effective and safe as mycophenolate mofetil (MMF) for patients after kidney transplantation."( Revival of effective and safe high-dose mizoribine for the kidney transplantation.
Doi, A; Hirakata, H; Kitada, H; Ota, M; Sugitani, A; Tanaka, M; Yoshida, J,
)
0.68
" Adverse drug reactions were reported in 18 patients, of whom 6 patients had to discontinue the study due to such adverse reactions; however, no serious adverse drug reactions definitely related to the study drug were noted."( Efficacy and safety of mizoribine for the treatment of Sjögren's syndrome: a multicenter open-label clinical trial.
Hashimoto, N; Ito, S; Kondo, H; Mimori, T; Minota, S; Nakayamada, S; Nara, H; Ogawa, N; Okada, J; Saito, K; Sano, H; Sugai, S; Sumida, T; Tanaka, Y; Umehara, H; Yoshifuji, H, 2007
)
0.65
"Mizoribine (MZR) is an immunosuppressant that inhibits nucleic acid metabolism and is a relatively safe disease-modifying anti-rheumatic drug (DMARD)."( Efficacy and safety of mizoribine by one single dose administration for patients with rheumatoid arthritis.
Aramaki, T; Arima, K; Eguchi, K; Fujikawa, K; Ichinose, K; Ida, H; Iwamoto, N; Kamachi, M; Kawakami, A; Kawashiri, SY; Nakamura, H; Origuchi, T; Tamai, M; Tsukada, T; Ueki, Y, 2010
)
2.11
" We show that MZR may be a useful and relatively safe therapy for patients in this group."( Efficacy and safety of mizoribine by one single dose administration for patients with rheumatoid arthritis.
Aramaki, T; Arima, K; Eguchi, K; Fujikawa, K; Ichinose, K; Ida, H; Iwamoto, N; Kamachi, M; Kawakami, A; Kawashiri, SY; Nakamura, H; Origuchi, T; Tamai, M; Tsukada, T; Ueki, Y, 2010
)
0.67
" With regard to safety, no serious adverse events were observed."( Efficacy and safety of single-dose mizoribine for patients with rheumatoid arthritis: results at 6 months after switching from a multiple-dose regimen without a change in total daily dose.
Haraoka, H; Kouchi, A; Matsushita, T; Nakajima, S; Nakamura, N; Nishimura, K; Nishino, J; Yokoe, I, 2011
)
0.65
" No serious adverse events occurred in any of the 3 groups."( Efficacy and safety of mizoribine combined with losartan in the treatment of IgA nephropathy: a multicenter, randomized, controlled study.
Chen, P; Chen, X; Huang, S; Li, Y; Lie, C; Liu, S; Miao, L; Wang, L; Wu, X; Xie, Y; Zhang, A, 2011
)
0.68
" Adverse events were recorded."( [Efficacy and safety of combination therapy with mizoribine and methotrexate for rheumatoid arthritis resistant with methotrexate].
Kawashima, M; Kimoto, O; Mukai, T; Ogawa, N; Ohashi, H; Sawada, J; Shimoyama, K; Suzuki, D; Yamamura, M, 2011
)
0.62
" MZ showed immunosuppressive effects in an experimental islet xenotransplantation model without adverse effects on endocrine function of islet grafts."( Mizoribine as sole immunosuppressive agent in islet xenotransplantation models: a candidate immunosuppressant causing no adverse effects on islets.
Gotoh, M; Ise, K; Ishii, S; Kenjo, A; Kimura, T; Oshibe, I; Saito, T; Satoh, Y; Shimizu, H; Yamashita, M, 2012
)
1.82
" Six patients experienced minor adverse events, including three minor infections."( Efficacy and safety of multitarget therapy with mizoribine and tacrolimus for systemic lupus erythematosus with or without active nephritis.
Kishimoto, M; Nomura, A; Ohara, Y; Okada, M; Rokutanda, R; Shimizu, H; Suyama, Y; Yamaguchi, K, 2012
)
0.63
"2 patient-years of follow-up, only one patient required discontinuation of MZR due to an adverse event."( Safety and efficacy of mizoribine in patients with connective tissue diseases other than rheumatoid arthritis.
Kishimoto, M; Nomura, A; Ohara, Y; Ohde, S; Okada, M; Rokutanda, R; Shimizu, H; Suyama, Y; Yamaguchi, K, 2014
)
0.71
" The safety of the study drug was assessed using the incidences of adverse events, drug discontinuations, and abnormal laboratory results."( Mizoribine versus mycophenolate mofetil in combination therapy with tacrolimus for de novo kidney transplantation: evaluation of efficacy and safety.
Cho, BH; Huh, KH; Joo, DJ; Ju, MK; Kang, CM; Kim, CD; Kim, SJ; Kim, YS; Lee, S; Park, KT; So, BJ, 2013
)
1.83
"MZR is an effective and safe immunosuppressive agent and high-dose MZR can be recommended as an alternative to MMF following adult renal transplantation in Asia, but hyperuricemia and liver damage should be closely monitored during the medication period."( Comparative efficacy and safety of mizoribine with mycophenolate mofetil for Asian renal transplantation--a meta-analysis.
Xing, S; Yang, J; Zhang, X; Zhou, P, 2014
)
0.68
" We previously reported that high-dose MZR, at 6 mg/kg/d, would be effective and safe for ABO-incompatible(ABO-i) living donor kidney transplantation (LDKT) patients when combined with cyclosporine (CsA) or tacrolimus(FK), anti-CD20 and anti-CD25 monoclonal antibodies, and corticosteroid without splenectomy in a 1-year study."( Usefulness and safety of high-dose mizoribine on ABO-incompatible living related kidney transplantation using anti-CD20 and anti-CD25 antibodies without splenectomy: 3-year results.
Harada, S; Ito, T; Koshino, K; Nakamura, T; Nakao, T; Nobori, S; Sakai, K; Suzuki, T; Ushigome, H; Yoshimura, N, 2014
)
0.68
"A high-dose MZR regimen including CNI (CsA or FK), steroid, and anti-CD20 and anti-CD25 antibodies without splenectomy was effective and safe in ABO-i renal transplantation."( Usefulness and safety of high-dose mizoribine on ABO-incompatible living related kidney transplantation using anti-CD20 and anti-CD25 antibodies without splenectomy: 3-year results.
Harada, S; Ito, T; Koshino, K; Nakamura, T; Nakao, T; Nobori, S; Sakai, K; Suzuki, T; Ushigome, H; Yoshimura, N, 2014
)
0.68
" The adverse responses were recorded."( Safety and efficacy of mizoribine treatment in nephrotic syndrome complicated with hepatitis B virus infection: a clinical study.
Ji, Y; Li, W; Liu, J; Sun, J; Wang, J; Yong, Q; Zhang, H; Zhang, K; Zhang, W, 2016
)
0.74
" We investigated whether high-dose MZR is effective and safe for renal transplant patients in conjunction with cyclosporine (CsA), basiliximab, and corticosteroids."( Efficacy and Safety of High-Dose Mizoribine Combined With Cyclosporine, Basiliximab, and Corticosteroids in Renal Transplantation: A Japanese Multicenter Study.
Akioka, K; Fujisawa, M; Fukuda, Y; Horimi, T; Ito, SI; Nakatani, T; Nishimura, K; Sugitani, A; Uchida, K; Ushigome, H; Yoshimura, N; Yuzawa, K, 2016
)
0.72
"Mizoribine (MZR) was effective and safe for living Chinese donor kidney transplantation (LDKT) on tacrolimus-based treatment 1 year after transplantation."( Efficacy and Safety of Mizoribine Combined With Tacrolimus in Living Donor Kidney Transplant Recipients: 3-Year Results by a Chinese Single Center Study.
Chen, XG; Liu, H; Shen, ZY; Shi, Y, 2019
)
2.27
" There were no significant differences in adverse events among the MZR or the MMF group, whereas the prevalence of gastrointestinal symptoms were significantly lower in the MZR treatment group (P = ."( Efficacy and Safety of Mizoribine Combined With Tacrolimus in Living Donor Kidney Transplant Recipients: 3-Year Results by a Chinese Single Center Study.
Chen, XG; Liu, H; Shen, ZY; Shi, Y, 2019
)
0.82
" We analyzed the Gastrointestinal Symptom Rating Scale (GSRS), estimated glomerular filtration rate (eGFR), graft rejection, serum creatinine, human leukocyte antigen (HLA) antibody, and the occurrence of adverse events among the 3 groups."( Efficacy and Safety of a Quadruple Regimen Compared with Triple Regimens in Patients with Mycophenolic Acid-Related Gastrointestinal Complications After Renal Transplantation: A Short-Term Single-Center Study.
Geng, L; Li, E; Peng, Z; Sun, H; Tian, J; Xian, W, 2020
)
0.56
" Disease exacerbation, GC dose, IgG-IgG4 titre and adverse events were evaluated using univariate analyses, including the Kaplan-Meier method."( Effectiveness and safety of mizoribine for the treatment of IgG4-related disease: a retrospective cohort study.
Fukui, S; Ikeda, Y; Kawaai, S; Kishimoto, M; Nakai, T; Nomura, A; Ohde, S; Okada, M; Suda, M; Tamaki, H, 2021
)
0.92
" We also assessed the relationship between the MZR concentrations and adverse events."( The efficacy and safety of mizoribine for maintenance therapy in patients with myeloperoxidase anti-neutrophil cytoplasmic antibody (MPO-ANCA)-associated vasculitis: the usefulness of serum mizoribine monitoring.
Arimura, Y; Fujimoto, S; Hirawa, N; Ito, T; Kobayashi, M; Makino, H; Mase, K; Matsuo, S; Muso, E; Nakagawa, N; Nitta, K; Saito, C; Usui, J; Wada, T; Yamagata, K; Yumura, W; Yuzawa, Y, 2022
)
1.02
" The treatment of one patient with C0 > 1 μg/mL was discontinued due to adverse events."( The efficacy and safety of mizoribine for maintenance therapy in patients with myeloperoxidase anti-neutrophil cytoplasmic antibody (MPO-ANCA)-associated vasculitis: the usefulness of serum mizoribine monitoring.
Arimura, Y; Fujimoto, S; Hirawa, N; Ito, T; Kobayashi, M; Makino, H; Mase, K; Matsuo, S; Muso, E; Nakagawa, N; Nitta, K; Saito, C; Usui, J; Wada, T; Yamagata, K; Yumura, W; Yuzawa, Y, 2022
)
1.02

Pharmacokinetics

Pharmacokinetic parameters for mizoribine were estimated using concentration-time profiles. The aim of this study was to investigate the pharmacokinetic variability of miz oribine in pediatric recipients of renal transplantation.

ExcerptReferenceRelevance
" Since the pharmacokinetics of prednisolone are little altered in renal transplantation, it is concluded that lymphocyte sensitivity specific to prednisolone may be a pharmacodynamic marker characteristic of successful graft survival in patients with histo-incompatibility and/or drug resistance."( Role of altered prednisolone-specific lymphocyte sensitivity in chronic renal failure as a pharmacodynamic marker of acute allograft rejection after kidney transplantation.
Hirano, T; Kang, XX; Kozaki, M; Oka, K; Sakurai, E; Tamaki, T, 1991
)
0.28
" An additional 10 mg/kg of mizoribine was administered once to both groups at the months of 6, 12, 18, 24, or 36 after the onset of this toxicological study so as to determine the pharmacokinetic behavior of serum mizoribine."( [Long-term toxicological studies with mizoribine (Bredinin) in beagle dogs (the first report). Blood chemistries, pharmacokinetics of mizoribine and fertility studies of the male dogs].
Maruyama, S; Masaki, Y; Taira, M; Uchida, H; Yasuda, S, 1985
)
0.84
"A pharmacokinetic study of bredinin, a new immunosuppressive agent, was carried out in 28 renal transplant patients."( Pharmacokinetics of bredinin in renal transplant patients.
Asada, S; Fukunishi, T; Ichikawa, Y; Nagano, S; Sonoda, T; Takada, K; Takahara, S, 1983
)
0.27
" Conclusions Based on the favourable safety profile and current pharmacokinetic information, a new starting dose in the 6-12 mg kg(-1) day(-1) range is recommended in the up to 3 months acute phase following transplantation, with dose reduction recommended only if the function of the transplanted kidney is impaired."( Safety, tolerability and pharmacokinetics of higher-dose mizoribine in healthy male volunteers.
Combs, M; Ishikawa, H; Obaidi, M; Stewart, AJ; Stypinski, D; Weber, M, 2007
)
0.58
"The population pharmacokinetic parameters of mizoribine in healthy subjects were estimated using a nonlinear mixed effects model (NONMEM) program."( Population pharmacokinetics of higher-dose mizoribine in healthy male volunteers.
Hashimoto, Y; Honda, M; Itoh, H; Suzuki, T, 2006
)
0.86
" We aimed at investigating the effect of high-doses of MZ on prevention of anti-donor antibody (Ab) production and acute Ab-mediated rejection (AMR) on the basis of the pharmacokinetic profile in a pig kidney transplantation model."( Prophylactic treatment of antibody-mediated rejection with high-dose mizoribine and pharmacokinetic study.
Kobayashi, T; Kuzuya, T; Liu, D; Ma, Y; Miwa, Y; Morozumi, K; Nagasaka, T; Nakao, A; Oikawa, T; Uchida, K; Yokoyama, I, 2007
)
0.57
" In addition, the method was successfully applied to estimate the pharmacokinetic parameters of mizoribine in Korean subjects following an oral administration of 100 mg mizoribine (two Bredinine 50 mg tablets)."( A simple HPLC method for the quantification of mizoribine in human serum: pharmacokinetic applications.
Choi, MS; Choi, SJ; Hur, HJ; Kuh, HJ; Lee, HJ; Lee, SB; Shin, YH, 2008
)
0.82
"Mizoribine (MZR) has been successfully used without serious adverse effects in patients with various types of glomerulonephritis, but there are only a few pharmacokinetic studies of MZR."( Pharmacokinetic study of mizoribine in child-onset glomerulonephritis.
Abe, Y; Fuke, T; Hisano, M; Itabashi, K; Mikawa, T; Tsuji, Y; Watanabe, S, 2008
)
2.09
" Pharmacokinetic parameters for mizoribine were estimated using concentration-time profiles."( Pharmacokinetic study of mizoribine in child-onset glomerulonephritis.
Abe, Y; Fuke, T; Hisano, M; Itabashi, K; Mikawa, T; Tsuji, Y; Watanabe, S, 2008
)
0.93
" In 4 of the 12 patients studied, kel decreased and the biological half-life (t1/2) of MZR was prolonged when co-administered with PRB, in comparison with the values when MZR was used alone, thus revealing that the PK of MZR was influenced by PRB."( Effects of probenecid on the pharmacokinetics of mizoribine and co-administration of the two drugs in patients with nephrotic syndrome.
Hara, Y; Hashimoto, Y; Hosoya, T; Ito, H; Miyazaki, Y; Okonogi, H; Utsunomiya, Y, 2010
)
0.62
"The aim of the present study was to estimate the population pharmacokinetic parameters of mizoribine in adult recipients of renal transplantation using a nonlinear mixed effects model (NONMEM) program."( Population pharmacokinetics of mizoribine in adult recipients of renal transplantation.
Hashimoto, Y; Ishibashi, M; Ishida, K; Okamoto, M, 2011
)
0.88
"The present findings suggested that not only the rate of renal excretion but also the extent of intestinal absorption of mizoribine is responsible for the large interindividual pharmacokinetic variability of the drug."( Population pharmacokinetics of mizoribine in adult recipients of renal transplantation.
Hashimoto, Y; Ishibashi, M; Ishida, K; Okamoto, M, 2011
)
0.86
" The aim of this study was to investigate the pharmacokinetic variability of mizoribine in pediatric recipients of renal transplantation."( Population pharmacokinetics of mizoribine in pediatric recipients of renal transplantation.
Hashimoto, Y; Ishida, K; Motoyama, O; Shishido, S; Tsuzuki, K, 2012
)
0.89
" The population pharmacokinetic parameters of mizoribine were estimated using a nonlinear mixed effects model program."( Population pharmacokinetics of mizoribine in pediatric recipients of renal transplantation.
Hashimoto, Y; Ishida, K; Motoyama, O; Shishido, S; Tsuzuki, K, 2012
)
0.92
"The present findings indicated that the rate of renal excretion and also the extent of intestinal absorption of mizoribine are responsible for the large interindividual pharmacokinetic variability of the drug."( Population pharmacokinetics of mizoribine in pediatric recipients of renal transplantation.
Hashimoto, Y; Ishida, K; Motoyama, O; Shishido, S; Tsuzuki, K, 2012
)
0.88
" In addition, the method was successfully applied to estimate the pharmacokinetic parameters of mizoribine in Chinese kidney transplant patients following an oral administration of 100 mg mizoribine (2 Bredinin® 50 mg tablets)."( Determination of mizoribine in human plasma using high-performance liquid chromatography: application to a pharmacokinetic study in Chinese renal transplant recipients.
Chen, X; Fu, XH; Huang, L; Ren, B; Wang, CX; Zhang, ZH, 2013
)
0.95
" Population pharmacokinetic analysis of MZR was performed based on serum concentration data."( Population pharmacokinetics of mizoribine in pediatric patients with kidney disease.
Fujieda, M; Gotoh, Y; Hashimoto, Y; Kaneda, H; Morooka, M; Nagai, T; Ohta, K; Satomura, K; Shimizu, M; Takaai, M; Uemura, O; Ushijima, K; Wada, N; Yamada, M; Yamada, T, 2016
)
0.72
" In addition, the population pharmacokinetic parameters obtained in this study are useful in determining the initial dosage or in the Bayesian analysis of mizoribine concentrations using scarce time points."( Population Pharmacokinetic Analysis of Mizoribine in Chinese Renal Transplant Recipients.
Chen, G; Chen, L; Deng, S; Fei, J; Fu, Q; Jiang, J; Li, J; Liu, L; Qiu, J; Ren, B; Wang, C; Zhang, H, 2018
)
0.95

Compound-Compound Interactions

Few have tried to prove the effectiveness of mizoribine combined with losartan for adult IgA nephropathy patients in a randomized controlled trial. To reduce the total dose of steroids, we have been using miz oribine (MZR) in combination with tonsillectomy-steroid pulse therapy since 2004.

ExcerptReferenceRelevance
" These results indicate that mizoribine in combination with IFN-alpha may have potential for the treatment of HCV infection."( Inhibition of bovine viral diarrhea virus (BVDV) by mizoribine: synergistic effect of combination with interferon-alpha.
Baba, C; Baba, M; Yanagida, K, 2004
)
0.87
"To evaluate the efficacy of prednisolone, warfarin, and dipyridamole therapy combined with mizoribine (PWDM) in the treatment of diffuse immunoglobulin A (IgA) nephropathy in comparison with prednisolone, warfarin, and dipyridamole therapy without mizoribine (PWD) and with methylprednisolone pulse therapy (PWD pulse)."( Efficacy of multidrug therapy combined with mizoribine in children with diffuse IgA nephropathy in comparison with multidrug therapy without mizoribine and with methylprednisolone pulse therapy.
Hosoya, M; Isome, M; Kawasaki, Y; Nozawa, R; Onishi, N; Suzuki, H; Suzuki, J; Takahashi, A,
)
0.61
" Since mizoribine is currently used in several clinical applications and has not been associated with severe side effects, mizoribine is considered to be of potential use as a new anti-HCV reagent in combination with IFN-alpha."( Mizoribine inhibits hepatitis C virus RNA replication: effect of combination with interferon-alpha.
Abe, K; Dansako, H; Ikeda, M; Kato, N; Naka, K, 2005
)
2.23
"The aim was to determine the efficacy of low-dose intermittent pulse administration of mizoribine (MZR), a purine synthesis inhibitor, in combination with methotrexate (MTX) to control the symptoms of rheumatoid arthritis (RA) in patients with an insufficient clinical response to MTX alone."( Effects of low-dose mizoribine pulse therapy in combination with methotrexate in rheumatoid arthritis patients with an insufficient response to methotrexate.
Ide, H; Isozaki, T; Kasama, T; Matsunawa, M; Miwa, Y; Negishi, M; Odai, T; Wakabayashi, K; Yajima, N, 2009
)
0.9
" To reduce the total dose of steroids, we have been using mizoribine (MZR) in combination with tonsillectomy-steroid pulse therapy since 2004."( Methylprednisolone pulse therapy combined with mizoribine following tonsillectomy for immunoglobulin A nephropathy: clinical remission rate, steroid sparing effect, and maintenance of renal function.
Fujino, T; Hirama, A; Iino, Y; Kaneko, T; Katayama, Y; Ueda, K; Utsumi, K, 2011
)
0.87
"Few have tried to prove the effectiveness of mizoribine combined with losartan for adult IgA nephropathy patients in a randomized controlled trial."( Efficacy and safety of mizoribine combined with losartan in the treatment of IgA nephropathy: a multicenter, randomized, controlled study.
Chen, P; Chen, X; Huang, S; Li, Y; Lie, C; Liu, S; Miao, L; Wang, L; Wu, X; Xie, Y; Zhang, A, 2011
)
0.94
"A multicenter, randomized, controlled, 12-month study was performed to evaluated the efficacy and safety of mizoribine combined with losartan for adult IgA nephropathy."( Efficacy and safety of mizoribine combined with losartan in the treatment of IgA nephropathy: a multicenter, randomized, controlled study.
Chen, P; Chen, X; Huang, S; Li, Y; Lie, C; Liu, S; Miao, L; Wang, L; Wu, X; Xie, Y; Zhang, A, 2011
)
0.89
"We performed a multicenter study in Japan to assess the efficacy and safety of immunosuppressive therapy with high-dose mizoribine (MZR; 6 mg/kg) combined with basiliximab (Bas), cyclosporine (CyA), and a corticosteroid in 90 patients."( Excellent results with high-dose mizoribine combined with cyclosporine, corticosteroid, and basiliximab in renal transplant recipients: multicenter study in Japan.
Akioka, K; Fujisawa, M; Fukuda, Y; Horimi, T; Ichikawa, Y; Ito, S; Nakatani, T; Nishimura, K; Sugitani, A; Uchida, K; Yoshimura, N; Yuzawa, K, 2012
)
0.87
" In our current treatment protocol, the total steroid dose has been significantly reduced through the use of the immunosuppressant mizoribine in combination with tonsillectomy-steroid pulse therapy for the treatment of active IgA nephropathy in patients with renal impairment."( Efficacy of steroid pulse therapy in combination with mizoribine following tonsillectomy for immunoglobulin A nephropathy in renally impaired patients.
Iino, Y; Kaneko, T; Katayama, Y; Shimizu, A; Tsuruoka, S, 2013
)
0.84
" One week later, intravenous methylprednisolone pulse therapy (500 mg/day) was administered for 3 days, followed by oral prednisolone in combination with mizoribine (100 to 150 mg/day)."( Efficacy of steroid pulse therapy in combination with mizoribine following tonsillectomy for immunoglobulin A nephropathy in renally impaired patients.
Iino, Y; Kaneko, T; Katayama, Y; Shimizu, A; Tsuruoka, S, 2013
)
0.84
"Steroid pulse therapy in combination with mizoribine following tonsillectomy is effective in improving urinary findings and preserving renal function in the treatment of IgA nephropathy, which remained active in patients with renal impairment (estimated glomerular filtration rate ≥20 and <60 mL/min/1."( Efficacy of steroid pulse therapy in combination with mizoribine following tonsillectomy for immunoglobulin A nephropathy in renally impaired patients.
Iino, Y; Kaneko, T; Katayama, Y; Shimizu, A; Tsuruoka, S, 2013
)
0.9
" Treatment protocols were a single-course steroid pulse combined with mizoribine during a period from August 2006 to June 2010 (Group A; n = 34) and a three-course steroid pulse during a period from July 2010 to March 2013 (Group B; n = 32)."( Comparison of immunosuppressive therapies for IgA nephropathy after tonsillectomy: three-course versus one-course steroid pulse combined with mizoribine.
Arai, M; Hirama, A; Ikeda, M; Kaneko, T; Morita, M; Shimizu, A; Tsuruoka, S; Watanabe, Y, 2015
)
0.85
"Single-course steroid pulse therapy combined with mizoribine was considered to have a protective effect on the renal function in IgA nephropathy, especially accompanying renal dysfunction."( Comparison of immunosuppressive therapies for IgA nephropathy after tonsillectomy: three-course versus one-course steroid pulse combined with mizoribine.
Arai, M; Hirama, A; Ikeda, M; Kaneko, T; Morita, M; Shimizu, A; Tsuruoka, S; Watanabe, Y, 2015
)
0.87
" This study was performed to compare two treatment regimens, steroid-pulse therapy or combined with mizoribine (MZR) in progressive IgAN."( Comparison of steroid-pulse therapy and combined with mizoribine in IgA nephropathy: a randomized controlled trial.
Hirakata, H; Hirakawa, M; Katafuchi, R; Kitazono, T; Masutani, K; Mitsuiki, K; Tsuchimoto, A; Tsuruya, K; Yamada, T, 2016
)
0.9
"Study design was a prospective randomized controlled trial of 40 patients with moderate to severe glomerular injuries who were randomly administered either pulse methylprednisolone followed by a 25-month course of oral prednisolone (P group, n = 20) or in combination with MZR (150 mg/day for 24 months, M + P group, n = 20)."( Comparison of steroid-pulse therapy and combined with mizoribine in IgA nephropathy: a randomized controlled trial.
Hirakata, H; Hirakawa, M; Katafuchi, R; Kitazono, T; Masutani, K; Mitsuiki, K; Tsuchimoto, A; Tsuruya, K; Yamada, T, 2016
)
0.68
" We could not find the additional effect of MZR in combination with steroid-pulses in this small-scale controlled trial."( Comparison of steroid-pulse therapy and combined with mizoribine in IgA nephropathy: a randomized controlled trial.
Hirakata, H; Hirakawa, M; Katafuchi, R; Kitazono, T; Masutani, K; Mitsuiki, K; Tsuchimoto, A; Tsuruya, K; Yamada, T, 2016
)
0.68
"Our objectives were to compare the clinical outcomes of mizoribine (12 mg/kg/d) and mycophenolate mofetil (2000 mg/d) in combination with tacrolimus, basiliximab, and corticosteroids."( A Prospective Randomized, Comparative Trial of High-Dose Mizoribine Versus Mycophenolate Mofetil in Combination With Tacrolimus and Basiliximab for Living Donor Renal Transplant: A Multicenter Trial.
Akiyama, T; Amada, N; Chikaraishi, T; Ishida, H; Takahara, S; Takahashi, K; Tanabe, K; Toma, H; Tomikawa, S; Uchida, K, 2016
)
0.93
" This prospective multi-institutional randomized comparative study compared mizoribine (n = 41) and mycophenolate mofetil (n = 42) in combination with tacrolimus, basiliximab, and corticosteroids for living-donor renal transplant recipients."( A Prospective Randomized, Comparative Trial of High-Dose Mizoribine Versus Mycophenolate Mofetil in Combination With Tacrolimus and Basiliximab for Living Donor Renal Transplant: A Multicenter Trial.
Akiyama, T; Amada, N; Chikaraishi, T; Ishida, H; Takahara, S; Takahashi, K; Tanabe, K; Toma, H; Tomikawa, S; Uchida, K, 2016
)
0.91
"A regimen of high-dose mizoribine in combination with calcineurin inhibitors basiliximab, and corticosteroids can provide effective immunosuppression while lowering the rate of cytomegalovirus infection in kidney transplant patients."( High-dose mizoribine combined with calcineurin inhibitor (cyclosporine or tacrolimus), basiliximab and corticosteroids for renal transplantation: A Japanese multicenter study.
Akioka, K; Kawakita, M; Nakamura, N; Nakatani, T; Nishimura, K; Nishioka, T; Ushigome, H; Watarai, Y; Yoshimura, N; Yuzawa, K, 2018
)
1.19
"We aimed to initially explore the efficiency and safety of mizoribine (MZR) combined with steroids and dietary sodium restriction on the treatment of primary membranous nephropathy (MN) compared with cyclophosphamide (CPM)-based steroids."( Mizoribine combined with steroids and dietary sodium restriction on the treatment of primary membranous nephropathy: a prospective study.
Chang, W; Sun, N; Wang, X; Zhang, M, 2023
)
2.6
" According to the therapy, they were divided into the MZR combined with steroids and dietary sodium restriction group (N = 30) and CPM-based steroids group (N = 30)."( Mizoribine combined with steroids and dietary sodium restriction on the treatment of primary membranous nephropathy: a prospective study.
Chang, W; Sun, N; Wang, X; Zhang, M, 2023
)
2.35
"Compared with the CPM-based steroids group, the MZR combined with steroids and dietary sodium restriction group had significantly lower daily sodium intake, serum sodium, blood pressure (BP), and 24 h urine protein (all P < 0."( Mizoribine combined with steroids and dietary sodium restriction on the treatment of primary membranous nephropathy: a prospective study.
Chang, W; Sun, N; Wang, X; Zhang, M, 2023
)
2.35
"This study demonstrates that MZR combined with steroids and dietary sodium restriction is superior to CPM-based steroids in terms of complete remission and 24 h urine protein in patients with primary MN."( Mizoribine combined with steroids and dietary sodium restriction on the treatment of primary membranous nephropathy: a prospective study.
Chang, W; Sun, N; Wang, X; Zhang, M, 2023
)
2.35

Bioavailability

Oral bioavailability of mizoribine was estimated by the recovery amount in the urine. Rats under cholestatic states exhibited significantly higher oral bioavailabilities than untreated control rats.

ExcerptReferenceRelevance
" The absorption rate of bredinin from the gastrointestinal (GI) tract was affected by GI diseases."( Pharmacokinetics of bredinin in renal transplant patients.
Asada, S; Fukunishi, T; Ichikawa, Y; Nagano, S; Sonoda, T; Takada, K; Takahara, S, 1983
)
0.27
" MMF was designed to enhance the oral bioavailability of the parent compound."( Mizoribine and mycophenolate mofetil.
Ishikawa, H, 1999
)
1.75
" The absorption rate in the most proximal segment of intestinal loop was the highest."( The nucleotide derivatives inosine and inosinic acid inhibit intestinal absorption of mizoribine in rats.
Fujioka, N; Nakanishi, T; Nakashima, M; Okada, M; Suzuki, K, 2006
)
0.56
" When mizoribine was administered orally in conscious rats, the bioavailability of mizoribine estimated by urinary excretion percentage of unchanged mizoribine was a dose dependent: 53."( Characterization of intestinal absorption of mizoribine mediated by concentrative nucleoside transporters in rats.
Kamio, Y; Mori, N; Murakami, T; Yokooji, T, 2008
)
1.09
" Oral bioavailability of mizoribine was obtained by dividing its amount in 24-hr urine by the daily dose."( Impact of concentrative nucleoside transporter 1 gene polymorphism on oral bioavailability of mizoribine in stable kidney transplant recipients.
Kagawa, Y; Kawakami, J; Mino, Y; Naito, T; Otsuka, A; Ozono, S; Tokashiki, S, 2010
)
0.88
" When oral bioavailability of mizoribine was estimated by the recovery amount in the urine, rats under cholestatic states exhibited significantly higher oral bioavailabilities than untreated control rats."( Increased intestinal absorption of mizoribine, an immunosuppressive agent, in cholestatic rats.
Kamio, Y; Mori, N; Murakami, T; Yokooji, T, 2010
)
0.93
"5-fold higher than that in control rats, whereas the bioavailability of cephalexin remained unchanged."( Modulation in concentrative nucleoside transporters-mediated intestinal absorption of mizoribine, an immunosuppressive agent, in lipopolysaccharide-treated rats.
Ishiguro, M; Kamio, Y; Mori, N; Murakami, T; Shimomukai, Y; Yokooji, T, 2011
)
0.59
"The aim of the present study was to investigate the genetic factors responsible for the interindividual variability in the bioavailability of mizoribine."( Effect of genetic polymorphisms of SLC28A1, ABCG2, and ABCC4 on bioavailability of mizoribine in healthy Japanese males.
Fukao, M; Hashimoto, Y; Ishida, K; Matsukura, H; Miyawaki, T; Sakamoto, T; Taguchi, M, 2011
)
0.8
" The aims of the present study were to investigate the cellular uptake of mizoribine in CNT1- and CNT2-expressing Madin-Darby canine kidney type II (MDCKII) cells, and to evaluate the effect of salt intake on bioavailability of mizoribine in healthy Japanese volunteers with SLC28A1 565-A/A and -G/A alleles."( Effect of salt intake on bioavailability of mizoribine in healthy Japanese males.
Fukao, M; Hashimoto, Y; Ishida, K; Matsukura, H; Miyawaki, T; Taguchi, M; Uemura, O; Unadkat, JD; Watanabe, H; Zhang, Z, 2013
)
0.88
" The absorption lag time, absorption rate constant, apparent distribution volume, and oral clearance were thereafter calculated and compared with the respective Japanese references."( Population Pharmacokinetic Analysis of Mizoribine in Chinese Renal Transplant Recipients.
Chen, G; Chen, L; Deng, S; Fei, J; Fu, Q; Jiang, J; Li, J; Liu, L; Qiu, J; Ren, B; Wang, C; Zhang, H, 2018
)
0.75
"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
)
0.51

Dosage Studied

Mizoribine (MIZ) suppressed the mitogen response and mixed lymphocyte reaction (MLR) significantly at doses of 100 micrograms/ml and 10 microgramS/ml in a dose-response analysis. Mizoribne (MZR) is an emerging treatment option for nephrotic syndrome. Its dosage and administration are yet lack of consensus.

ExcerptRelevanceReference
" In order to determine the ideal form of induction regimen, combination drugs with CYA, the initial dosage of CYA and its blood trough level were retrospectively analyzed with particular reference to the possible factors relevant to the occurrence of acute rejection episode in the first three post-transplant months and graft survival."( [Study of 54 renal allograft recipients in the cyclosporin A era. What influences acute rejection episode and long-term graft survival?].
Chikaraishi, T; Hirano, T; Kanagawa, K; Koyanagi, T; Seki, T; Takeuchi, I; Tanda, K; Togashi, M; Tsubo, S, 1992
)
0.28
" In the dose-response experiments, one eye of each rabbit was treated topically with Bredinin, and the other eye with vehicle immediately after deepithelialization."( The suppression of acute corneal inflammation by Bredinin.
Carter, JM; Gebhardt, BM; Kaufman, HE; Kissling, GE, 1987
)
0.27
"Mizoribine (MIZ) suppressed the mitogen response and mixed lymphocyte reaction (MLR) significantly at doses of 100 micrograms/ml and 10 micrograms/ml in a dose-response analysis."( The immunosuppressive mode of action of mizoribine.
Arima, M; Ichikawa, Y; Ihara, H; Ishibashi, M; Sagawa, S; Shrestha, GR; Sonoda, T; Takada, K; Takahara, S, 1984
)
1.98
" In this trial, the combination therapy was effective for the decrease of urinary protein in one case, and for the reduction of a dosage of oral PSL in one case."( [Effects of combined administration of prednisolone and mizoribine in the course of remission for SLE children with nephritis].
Aihara, Y; Ibe, M; Kuriyama, T; Mitsuda, T; Mori, M; Shimizu, C; Takahashi, Y; Yokota, S, 1994
)
0.53
"We evaluated a 1-year course of a newly developed immunosuppressant, mizoribine (at a dosage of 3 mg/kg body weight per day), in nine children with steroid-dependent nephrotic syndrome."( Mizoribine in steroid-dependent nephrotic syndrome of childhood.
Hamasaki, T; Kinoshita, Y; Mori, M; Saeki, T; Sakano, T, 1997
)
1.97
" In this study, we examined the dosing time-dependent alterations in the pharmacokinetics and pharmacodynamics of Miz."( Dosing time-dependent pharmacological effects of anti-metabolites for rat cardiac graft.
Fujimura, A; Higuchi, S; Hishikawa, S; Kobayashi, E; Sudoh, T; Sugimoto, K; Sunaga, K; To, H; Uchida, H; Xiu, DR, 2001
)
0.31
" The efficacy of MZR was evaluated by the changes from baseline values of serum C3, serum C4, anti-dsDNA antibody titer, erythrocyte sedimentation rate (ESR), urinary protein, dosage of prednisolone (PSL), and the sum of the scores defined by these parameters."( Efficacy of mizoribine in the treatment of systemic lupus erythematosus in children.
Imanaka, H; Kawano, Y; Maeno, N; Ohkawa, T; Takei, S; Yoshidome, K, 2004
)
0.7
" The clinical dosage of MZ (2-5 mg/kg) is much lower than that of MMF (20-60 mg/kg)."( Potential value of high-dose mizoribine as rescue therapy for ongoing acute humoral rejection.
Kobayashi, T; Kuzuya, T; Liu, D; Ma, Y; Miwa, Y; Morozumi, K; Nagasaka, T; Nakao, A; Oikawa, T; Shimano, Y; Takeuchi, O; Uchida, K; Yokoyama, I, 2005
)
0.62
" Therefore, the mizoribine concentration in blood should be monitored and the dosage adjusted, depending on the condition of renal function."( A simple determination of mizoribine in human plasma by liquid chromatography with UV detection.
Inukai, Y; Kaji, H; Maiguma, T; Makino, K; Ono, H; Tagawa, Y; Taniguchi, R; Teshima, D,
)
0.78
" Other IMP dehydrogenase inhibitors administered near maximum tolerated doses using the same dosing regimen as for ribavirin were found to slightly enhance virus replication in the lungs."( Enhancement of the infectivity of SARS-CoV in BALB/c mice by IMP dehydrogenase inhibitors, including ribavirin.
Bailey, K; Barnard, DL; Carson, DA; Cottam, HB; Day, CW; Heiner, M; Hoopes, J; Lauridsen, L; Lee, J; Li, JK; Montgomery, R; Sidwell, RW; Winslow, S, 2006
)
0.33
" Previous reports suggested that modification of MZR therapy with a total dosage and administration schedule may improve the therapeutic effect."( [Beneficial and adverse effects of high-dosage MZR therapy in the management of children with frequently relapsing nephrotic syndrome].
Goto, M; Hamasaki, Y; Hataya, H; Honda, M; Ikeda, M; Ishikura, K, 2006
)
0.33
" It has been postulated that as renal function returns to normal, higher doses may be needed to maintain efficacy than the current clinical dosage of 2-5 mg kg(-1) day(-1)."( Safety, tolerability and pharmacokinetics of higher-dose mizoribine in healthy male volunteers.
Combs, M; Ishikawa, H; Obaidi, M; Stewart, AJ; Stypinski, D; Weber, M, 2007
)
0.58
"Although mizoribine (MZ), which inhibits inosine monophosphate dehydrogenase in the same way as mycophenolate mofetil, recently proved more effective when higher doses were administered than previously approved, neither the optimal dosage nor blood concentration has yet been clarified."( Prophylactic treatment of antibody-mediated rejection with high-dose mizoribine and pharmacokinetic study.
Kobayashi, T; Kuzuya, T; Liu, D; Ma, Y; Miwa, Y; Morozumi, K; Nagasaka, T; Nakao, A; Oikawa, T; Uchida, K; Yokoyama, I, 2007
)
0.99
" The dosage of prednisolone could be tapered from 24."( Mizoribine therapy for patients with lupus nephritis: the association between peak mizoribine concentration and clinical efficacy.
Ajiro, J; Gejyo, F; Hasegawa, H; Hirose, S; Ito, S; Kuroda, T; Murakami, S; Nakano, M; Nakatsue, T; Sakatsume, M; Sato, H; Tanabe, N; Wada, Y, 2007
)
1.78
" Thereafter, when tapering the dosage from 60 to 30 mg/day, the lupus nephritis flared up and he was re-hospitalized in February of 2001."( A case of lupus nephritis improved after appropriately adjusting the dosage of mizoribine.
Fukuda, W; Hamaguchi, M; Ishino, H; Kadoya, M; Kawahito, Y; Kohno, M; Niimi, M; Tsubouchi, Y; Wada, M; Yamamoto, A; Yoshikawa, T, 2008
)
0.57
" The therapeutic benefits of MZB pulse therapy were assessed based on a comparison of the incidence of relapse (times/year) and the required daily dosage of prednisolone (PSL) before and after therapy."( Effect of oral mizoribine pulse therapy for frequently relapsing steroid-dependent nephrotic syndrome.
Fujieda, M; Hayashi, A; Ishihara, M; Morita, T; Ohta, T; Sakano, T; Utsunomiya, Y; Wakiguchi, H, 2008
)
0.7
"05), and the required daily dosage of PSL after therapy was lower than that before therapy (0."( Effect of oral mizoribine pulse therapy for frequently relapsing steroid-dependent nephrotic syndrome.
Fujieda, M; Hayashi, A; Ishihara, M; Morita, T; Ohta, T; Sakano, T; Utsunomiya, Y; Wakiguchi, H, 2008
)
0.7
"Our results show that MZB pulse therapy is effective in decreasing the frequency of relapse and reducing the required PSL dosage in older pediatric patients with FR-SDNS."( Effect of oral mizoribine pulse therapy for frequently relapsing steroid-dependent nephrotic syndrome.
Fujieda, M; Hayashi, A; Ishihara, M; Morita, T; Ohta, T; Sakano, T; Utsunomiya, Y; Wakiguchi, H, 2008
)
0.7
" Co-administration of PRB with MZR appears to be effective in prolonging the biological half-life of MZR and enhancing its effect in patients with nephrotic syndrome, although further studies will be required to determine the optimal dosage of PRB and renoprotective effects."( Effects of probenecid on the pharmacokinetics of mizoribine and co-administration of the two drugs in patients with nephrotic syndrome.
Hara, Y; Hashimoto, Y; Hosoya, T; Ito, H; Miyazaki, Y; Okonogi, H; Utsunomiya, Y, 2010
)
0.62
"The efficacy of mizoribine (MZR) in treatment of rheumatoid arthritis (RA) was retrospectively investigated in terms of drug survival, improvement in Disease Activity Score-28 (DAS28)-C-reactive protein (CRP), and blood MZR concentration obtained 3 h after dosing (MZR-C3)."( An investigation of the correlation between blood concentration of mizoribine and its efficacy in treatment of rheumatoid arthritis based on indices of drug survival and improvement in DAS28-CRP.
Akimoto, M; Arishima, Y; Eiraku, N; Izumihara, T; Matsuda, T; Ohkura, S; Ohtsubo, H; Sunahara, N; Yoshitama, T, 2012
)
0.96
"To compare the efficacy of MZR administered via different regimens, the subjects were divided into 2 groups: those receiving a single dose of MZR at 100-150 mg every other day (group A) and those receiving 2 or 3 divided doses of the drug on consecutive days, which is the usual dosing method of the drug (group B)."( An investigation of the correlation between blood concentration of mizoribine and its efficacy in treatment of rheumatoid arthritis based on indices of drug survival and improvement in DAS28-CRP.
Akimoto, M; Arishima, Y; Eiraku, N; Izumihara, T; Matsuda, T; Ohkura, S; Ohtsubo, H; Sunahara, N; Yoshitama, T, 2012
)
0.62
"We investigated the efficacy of a high-dose intermittent dosing treatment method (weekly mizoribine pulse therapy) conceived in the hope of achieving better efficacy by increasing the peak blood levels of mizoribine in patients with refractory lupus nephritis."( Efficacy of weekly mizoribine pulse therapy in refractory lupus nephritis.
Amano, K; Ito, T; Kameda, H; Kondo, T; Kurasawa, T; Nagasawa, H; Nishi, E; Nishimura, K; Ogawa, H; Okuyama, A; Sakai, R; Shirai, Y; Takei, H; Takeuchi, T, 2013
)
0.94
" The therapeutic benefits of MZB pulse therapy were assessed based on a comparison of the incidence of relapse and the required daily dosage of prednisolone (PSL) in the 12 months prior to and following therapy."( Effect of single-dose oral mizoribine pulse therapy twice per week for frequently relapsing steroid-dependent nephrotic syndrome.
Fujieda, M; Hayashi, A; Ishihara, M; Morita, T; Ohta, T; Okada, S; Sakano, T; Wakiguchi, H, 2012
)
0.68
"01) and the required daily dosage of prednisolone (PSL) after therapy was lower than that before therapy (0."( Effect of single-dose oral mizoribine pulse therapy twice per week for frequently relapsing steroid-dependent nephrotic syndrome.
Fujieda, M; Hayashi, A; Ishihara, M; Morita, T; Ohta, T; Okada, S; Sakano, T; Wakiguchi, H, 2012
)
0.68
"Individual dosing is required to optimize C(max) in childhood-onset glomerular disease patients."( Mizoribine requires individual dosing due to variation of bioavailability.
Abe, Y; Fuke, T; Hibino, S; Itabashi, K; Murayama, J; Nakano, Y; Saito, T; Sakurai, S; Takeshi, M; Watanabe, S, 2012
)
1.82
"Mizoribine (MZR) was approved in 1984 in Japan for the suppression of rejection in renal transplantation with an approved administration dosage of 1-3 mg/kg/day."( Randomized comparative trial of mizoribine versus mycophenolate mofetil in combination with tacrolimus for living donor renal transplantation.
Akiyama, T; Amada, N; Takahara, S; Takahashi, K; Tanabe, K; Toma, H; Uchida, K, 2013
)
2.12
" The dosage of prednisone and/or mizoribine was tapered according to the urinary protein-to-creatinine ratio (P/C)."( Efficacy of mizoribine followed by low-dose prednisone in patients with idiopathic membranous nephropathy and nephrotic-range proteinuria.
Matsumoto, Y; Moriki, T; Nojima, Y; Shimada, Y, 2013
)
1.05
" Subgroup analysis was conducted according to the administration dosage of MZR."( Comparative efficacy and safety of mizoribine with mycophenolate mofetil for Asian renal transplantation--a meta-analysis.
Xing, S; Yang, J; Zhang, X; Zhou, P, 2014
)
0.68
" After adding MZR, we successfully tapered the orally dosed prednisolone without recurrent fever or complications."( A case of microscopic polyangiitis in an elderly patient presenting predominantly with cholecystitis successfully treated with mizoribine.
Ichinose, K; Iwanaga, N; Kawakami, A; Nakamura, H; Okada, A; Origuchi, T; Tamai, M; Yamasaki, S, 2014
)
0.61
"To evaluate the correlation between the efficacy of mizoribine (MZR) and the factors that might effect MZR concentration: renal function and dosage and administration of MZR in patients with rheumatoid arthritis (RA)."( The efficacy of mizoribine for the treatment of rheumatoid arthritis and its correlation with renal function.
Amano, K; Aoki, K; Azuma, T; Chino, K; Handa, Y; Hirose, T; Hoshi, K; Kaneko, M; Kawagoe, M; Kida, I; Kobayashi, S; Kuga, Y; Matsui, T; Matsuzaki, T; Mimura, T; Moriguchi, M; Nakajima, K; Nishi, E; Okuyama, A; Ota, M; Sakurai, T; Suzuki, K; Terai, C; Tsutsumi, T; Yoshida, H, 2014
)
1
" To obtain the expected clinical efficacy, the regular MZR dosage schedule (2-3 mg/kg/day) might be insufficient for pediatric patients."( Population pharmacokinetics of mizoribine in pediatric patients with kidney disease.
Fujieda, M; Gotoh, Y; Hashimoto, Y; Kaneda, H; Morooka, M; Nagai, T; Ohta, K; Satomura, K; Shimizu, M; Takaai, M; Uemura, O; Ushijima, K; Wada, N; Yamada, M; Yamada, T, 2016
)
0.72
"Everolimus (EVR) has been used widely for the purpose of reducing the dosage of calcineurin inhibitor (CNI), leading to decreasing CNI nephrotoxicity."( Effectiveness of the Combination of Everolimus and Tacrolimus With High Dosage of Mizoribine for Living Donor-Related Kidney Transplantation.
Harada, S; Ito, T; Koshino, K; Nakamura, T; Nakao, T; Nobori, S; Suzuki, T; Ushigome, H; Yoshimura, N, 2016
)
0.66
" Calcineurin inhibitor (CNI) dosage was reduced and renal function improved, and mean estimated glomerular filtration rate recovered from 42."( Experience of Quatro-Therapy With Everolimus to Minimize Calcineurin Inhibitor for Kidney Transplant Recipients.
Furuya, R; Irie, S; Matsuoka, H; Matsuzaki, H; Miyajima, S; Miyazaki, T; Nakamura, N; Tanaka, M,
)
0.13
" The oral steroid dosage decreased from baseline to 24 months."( Post-marketing surveillance study of the long-term use of mizoribine for the treatment of lupus nephritis: 2-Year results.
Okada, K; Takeuchi, T; Yagi, N; Yoshida, H, 2018
)
0.73
" Immunosuppression used cyclosporine (88) or tacrolimus (68) as a calcineurin inhibitor, and the dosage was adjusted based on blood concentrations."( High-dose mizoribine combined with calcineurin inhibitor (cyclosporine or tacrolimus), basiliximab and corticosteroids for renal transplantation: A Japanese multicenter study.
Akioka, K; Kawakita, M; Nakamura, N; Nakatani, T; Nishimura, K; Nishioka, T; Ushigome, H; Watarai, Y; Yoshimura, N; Yuzawa, K, 2018
)
0.88
" In addition, the population pharmacokinetic parameters obtained in this study are useful in determining the initial dosage or in the Bayesian analysis of mizoribine concentrations using scarce time points."( Population Pharmacokinetic Analysis of Mizoribine in Chinese Renal Transplant Recipients.
Chen, G; Chen, L; Deng, S; Fei, J; Fu, Q; Jiang, J; Li, J; Liu, L; Qiu, J; Ren, B; Wang, C; Zhang, H, 2018
)
0.95
" Mizoribine (MZR) is an emerging treatment option for nephrotic syndrome; however, its dosage and administration are yet lack of consensus."( Effect of mizoribine pulse therapy in adult membranous nephropathy.
Chang, W; Han, Y; Liu, Y; Wang, X; Zhang, M; Zhang, W, 2021
)
1.93
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (1)

RoleDescription
anticoronaviral agentAny antiviral agent which inhibits the activity of coronaviruses.
[role 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]

Drug Classes (1)

ClassDescription
imidazolesA five-membered organic heterocycle containing two nitrogen atoms at positions 1 and 3, or any of its derivatives; compounds containing an imidazole skeleton.
[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 (25)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency39.81070.177814.390939.8107AID2147
acetylcholinesteraseHomo sapiens (human)Potency0.77620.002541.796015,848.9004AID1347398
GLS proteinHomo sapiens (human)Potency5.62340.35487.935539.8107AID624146
GLI family zinc finger 3Homo sapiens (human)Potency6.49170.000714.592883.7951AID1259369; AID1259392
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency31.62280.011212.4002100.0000AID1030
regulator of G-protein signaling 4Homo sapiens (human)Potency0.33590.531815.435837.6858AID504845
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency30.90080.01237.983543.2770AID1645841
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency29.84930.003041.611522,387.1992AID1159552; AID1159555
retinoid X nuclear receptor alphaHomo sapiens (human)Potency0.04770.000817.505159.3239AID1159527
arylsulfatase AHomo sapiens (human)Potency8.49211.069113.955137.9330AID720538
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency32.46480.035520.977089.1251AID504332
Bloom syndrome protein isoform 1Homo sapiens (human)Potency0.00280.540617.639296.1227AID2364; AID2528
lysosomal alpha-glucosidase preproproteinHomo sapiens (human)Potency8.84450.036619.637650.1187AID2100
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency6.30963.548119.542744.6684AID743266
huntingtin isoform 2Homo sapiens (human)Potency0.56230.000618.41981,122.0200AID1688
peptidyl-prolyl cis-trans isomerase NIMA-interacting 1Homo sapiens (human)Potency0.95280.425612.059128.1838AID504536
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency4.46680.050127.073689.1251AID588590
survival motor neuron protein isoform dHomo sapiens (human)Potency0.03550.125912.234435.4813AID1458
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency26.65140.251215.843239.8107AID504327
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency8.49210.060110.745337.9330AID485368
[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)
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)133.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)133.00000.20005.677410.0000AID1473741
Bile salt export pumpHomo sapiens (human)IC50 (µMol)133.00000.11007.190310.0000AID1473738
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
glycogen synthase kinase-3 beta isoform 1Homo sapiens (human)EC50 (µMol)300.00000.212522.156283.9400AID434954
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (41)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of gene expressionCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bile acid and bile salt transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
heme catabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic export from cellCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transepithelial transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
leukotriene transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
monoatomic anion transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (24)

Processvia Protein(s)Taxonomy
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
protein bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
organic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type xenobiotic transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP hydrolysis activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (17)

Processvia Protein(s)Taxonomy
plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell surfaceCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
intercellular canaliculusCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (89)

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.
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.
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.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The 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.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings 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.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical 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.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The 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.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS 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.
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.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
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.
AID588378qHTS for Inhibitors of ATXN expression: Validation
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID102505In vitro inhibitory activity against growth of Human gaint cell carcinoma (Lu-65) cells1991Journal of medicinal chemistry, Feb, Volume: 34, Issue:2
Nucleosides and nucleotides. 96. Synthesis and antitumor activity of 5-ethynyl-1-beta-D-ribofuranosylimidazole-4-carboxamide (EICAR) and its derivatives.
AID977599Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID147783In vitro inhibitory activity against growth of Human osteosarcoma (OST) cells1991Journal of medicinal chemistry, Feb, Volume: 34, Issue:2
Nucleosides and nucleotides. 96. Synthesis and antitumor activity of 5-ethynyl-1-beta-D-ribofuranosylimidazole-4-carboxamide (EICAR) and its derivatives.
AID290453Selectivity index, ratio of CC50 for Vero E6 cells to IC50 for SARS-CoV Frankfurt12007Bioorganic & medicinal chemistry letters, May-01, Volume: 17, Issue:9
Synthesis and biological evaluation of nucleoside analogues having 6-chloropurine as anti-SARS-CoV agents.
AID1473738Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1473741Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID201697In vitro inhibitory activity against growth of Human colon adenocarcinoma (SW-480) cells1991Journal of medicinal chemistry, Feb, Volume: 34, Issue:2
Nucleosides and nucleotides. 96. Synthesis and antitumor activity of 5-ethynyl-1-beta-D-ribofuranosylimidazole-4-carboxamide (EICAR) and its derivatives.
AID977602Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID95853In vitro inhibitory activity against growth of Human oral epidermoid carcinoma (KB) cells1991Journal of medicinal chemistry, Feb, Volume: 34, Issue:2
Nucleosides and nucleotides. 96. Synthesis and antitumor activity of 5-ethynyl-1-beta-D-ribofuranosylimidazole-4-carboxamide (EICAR) and its derivatives.
AID521220Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay2007Nature chemical biology, May, Volume: 3, Issue:5
Chemical genetics reveals a complex functional ground state of neural stem cells.
AID155866In vitro inhibitory activity against growth of Human large-cell carcinoma (PC-13) cells1991Journal of medicinal chemistry, Feb, Volume: 34, Issue:2
Nucleosides and nucleotides. 96. Synthesis and antitumor activity of 5-ethynyl-1-beta-D-ribofuranosylimidazole-4-carboxamide (EICAR) and its derivatives.
AID209963In vitro inhibitory activity against growth of Human bladder transitional-cell carcinoma (T-24) cells1991Journal of medicinal chemistry, Feb, Volume: 34, Issue:2
Nucleosides and nucleotides. 96. Synthesis and antitumor activity of 5-ethynyl-1-beta-D-ribofuranosylimidazole-4-carboxamide (EICAR) and its derivatives.
AID290452Cytotoxicity against Vero E6 cells2007Bioorganic & medicinal chemistry letters, May-01, Volume: 17, Issue:9
Synthesis and biological evaluation of nucleoside analogues having 6-chloropurine as anti-SARS-CoV agents.
AID1473739Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID85450In vitro inhibitory activity against growth of Human fibrosarcoma (HT1080) cells1991Journal of medicinal chemistry, Feb, Volume: 34, Issue:2
Nucleosides and nucleotides. 96. Synthesis and antitumor activity of 5-ethynyl-1-beta-D-ribofuranosylimidazole-4-carboxamide (EICAR) and its derivatives.
AID1473740Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID290451Antiviral activity against SARS-CoV Frankfurt1 in Vero E6 cells by plaque reduction assay2007Bioorganic & medicinal chemistry letters, May-01, Volume: 17, Issue:9
Synthesis and biological evaluation of nucleoside analogues having 6-chloropurine as anti-SARS-CoV agents.
AID156170In vitro inhibitory activity against growth of Human lung adenocarcinoma (PC-3) cells.1991Journal of medicinal chemistry, Feb, Volume: 34, Issue:2
Nucleosides and nucleotides. 96. Synthesis and antitumor activity of 5-ethynyl-1-beta-D-ribofuranosylimidazole-4-carboxamide (EICAR) and its derivatives.
AID156356In vitro inhibitory activity against growth of Human lung small-cell carcinoma (PC-6) cells1991Journal of medicinal chemistry, Feb, Volume: 34, Issue:2
Nucleosides and nucleotides. 96. Synthesis and antitumor activity of 5-ethynyl-1-beta-D-ribofuranosylimidazole-4-carboxamide (EICAR) and its derivatives.
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.
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.
AID1224864HCS microscopy assay (F508del-CFTR)2016PloS one, , Volume: 11, Issue:10
Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (562)

TimeframeStudies, This Drug (%)All Drugs %
pre-199069 (12.28)18.7374
1990's131 (23.31)18.2507
2000's144 (25.62)29.6817
2010's190 (33.81)24.3611
2020's28 (4.98)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 36.93

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

MetricThis Compound (vs All)
Research Demand Index36.93 (24.57)
Research Supply Index6.49 (2.92)
Research Growth Index4.73 (4.65)
Search Engine Demand Index54.12 (26.88)
Search Engine Supply Index1.97 (0.95)

This Compound (36.93)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials75 (12.84%)5.53%
Reviews55 (9.42%)6.00%
Case Studies102 (17.47%)4.05%
Observational3 (0.51%)0.25%
Other349 (59.76%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (6)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Multi-center, Randomized, Controlled, Open-label Clinical Study to Evaluate the Efficacy and Safety of Mizoribine in Comparison With Cyclophosphamide in the Treatment of Lupus Nephritis [NCT02256150]Phase 3250 participants (Actual)Interventional2014-11-30Completed
A Randomized, Double-blind, Multicenter Study Evaluating the Safety and Efficacy of Sarilumab Added to Non-MTX DMARDs or as Monotherapy in Japanese Patients With Active Rheumatoid Arthritis [NCT02373202]Phase 391 participants (Actual)Interventional2015-02-28Completed
A Multi-center, Randomized, Controlled, Open-label Clinical Study to Evaluate the Efficacy and Safety of Mizoribine in Comparison With Cyclophosphamide in the Treatment of Refractory Nephrotic Syndrome [NCT02257697]Phase 3239 participants (Actual)Interventional2014-11-30Completed
Open Label, Multicenter, Randomized Study to Assess the Efficacy and Safety of Mizoribine in Active Rheumatoid Arthritis Patients Unsuccessfully Treated With Disease-modifying Antirheumatic Drug [NCT02005757]Phase 260 participants (Anticipated)Interventional2013-11-30Recruiting
Comparative Efficacy of Mizoribine With Mycophenolate Mofetil for Living Related Kidney Transplantation Recipients [NCT06114953]Phase 4152 participants (Anticipated)Interventional2023-01-01Recruiting
An Open Study on the Preventive Effect of Early Mizoribine Conversion on BKV Nephropathy in Renal Transplant Recipients [NCT05293704]Phase 430 participants (Anticipated)Interventional2022-05-01Not yet recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT02373202 (11) [back to overview]Change From Baseline at Week 52 in Disease Activity Score for 28 Joints Based on C-Reactive Protein (DAS28-CRP)
NCT02373202 (11) [back to overview]Change From Baseline in Health Assessment Questionnaire-Disability Index (HAQ-DI) Score at Week 52
NCT02373202 (11) [back to overview]Number of Participants With Potentially Clinically Significant Electrocardiogram (ECG) Abnormalities
NCT02373202 (11) [back to overview]Number of Participants With Potentially Clinically Significant Laboratory Abnormalities: Electrolytes
NCT02373202 (11) [back to overview]Number of Participants With Potentially Clinically Significant Laboratory Abnormalities: Hematological Parameters
NCT02373202 (11) [back to overview]Number of Participants With Potentially Clinically Significant Laboratory Abnormalities: Liver Function Parameters
NCT02373202 (11) [back to overview]Number of Participants With Potentially Clinically Significant Laboratory Abnormalities: Metabolic Parameters
NCT02373202 (11) [back to overview]Number of Participants With Potentially Clinically Significant Laboratory Abnormalities: Renal Function Parameters
NCT02373202 (11) [back to overview]Number of Participants With Potentially Clinically Significant Vital Signs Abnormalities
NCT02373202 (11) [back to overview]Number of Participants With Treatment-Emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)
NCT02373202 (11) [back to overview]Percentage of Participants Achieving American College of Rheumatology (ACR) 20, 50 and 70 Responses at Week 52

Change From Baseline at Week 52 in Disease Activity Score for 28 Joints Based on C-Reactive Protein (DAS28-CRP)

DAS28-CRP is a composite score that contains 4 variables: TJC (based on 28 joints), SJC (based on 28 joints), participant's assessment of general health on VAS (range 0 [very well] to 100 mm [extremely bad]) and CRP (mg/L). DAS28-CRP total score ranges from 2-10 with a lower score indicating less disease activity. A DAS28-CRP above 5.1 indicates high disease activity, whereas below 3.2 indicates low disease activity and below 2.6 as disease remission. (NCT02373202)
Timeframe: Baseline, Week 52

Interventionunits on a scale (Mean)
Sarilumab 150 mg q2w + DMARDs-2.90
Sarilumab 200 mg q2w + DMARDs-2.47
Sarilumab 150 mg q2w-2.62
Sarilumab 200 mg q2w-2.64

[back to top]

Change From Baseline in Health Assessment Questionnaire-Disability Index (HAQ-DI) Score at Week 52

HAQ-DI assessed the degree of difficulty participants experienced in 8 daily living activity domains during a week: dressing/grooming, arising, eating, walking, hygiene, reach, grip, and other activities. Each activity category consisted of 2-3 items. Each items's difficulty was scored from 0-3 (0=no difficulty, 1=some difficulty, 2=much difficulty, 3=unable to do). Overall HAQ-DI score was computed as the sum of domain scores divided by the number of domains answered, providing a score from 0-3. Low scores denoted improvement of disability/lower degree of domain difficulty. (NCT02373202)
Timeframe: Baseline, Week 52

Interventionunits on a scale (Mean)
Sarilumab 150 mg q2w + DMARDs-0.52
Sarilumab 200 mg q2w + DMARDs-0.34
Sarilumab 150 mg q2w-0.48
Sarilumab 200 mg q2w-0.38

[back to top]

Number of Participants With Potentially Clinically Significant Electrocardiogram (ECG) Abnormalities

"Criteria for potentially clinically significant ECG abnormalities:~PR Interval: >200 milliseconds (ms); >200 ms and IFB >=25%; >220 ms; >220 ms and IFB >=25%; >240 ms; >240 ms and IFB >=25%~QRS Interval: >110 ms; >110 ms and IFB >=25%; >120 ms; >120 ms and IFB >=25%~QT Interval: >500 ms~QTc Bazett (QTc B): >450 ms; >480 ms; >500 ms; IFB >30 and <=60 ms, IFB >60 ms~QTc Fridericia (QTc F): >450 ms; >480 ms; >500 ms; IFB >30 and <=60 ms; IFB >60 ms" (NCT02373202)
Timeframe: Baseline up to Week 58

,,,
Interventionparticipants (Number)
PR >200 msPR >200 ms and IFB >=25%PR >220 msPR >220 ms and IFB >=25%PR >240 msPR >240 ms and IFB >=25%QRS >110 msQRS >110 ms and IFB >=25%QRS >120 msQRS >120 ms and IFB >=25%QT >500 msQTc B >450 msQTc B >480 msQTc B >500 msQTc B IFB >30 and <=60 msQTc B IFB >60 msQTc F >450 msQTc F >480 msQTc F >500 msQTc F IFB >30 and <=60 msQTc F IFB >60 ms
Sarilumab 150 mg q2w000000000006002020000
Sarilumab 150 mg q2w + DMARDs000000000002000020000
Sarilumab 200 mg q2w1010001000110101061000
Sarilumab 200 mg q2w + DMARDs000000202001101010000

[back to top]

Number of Participants With Potentially Clinically Significant Laboratory Abnormalities: Electrolytes

"Criteria for potentially clinically significant abnormalities:~Sodium: <=129 mmol/L; >=160 mmol/L~Potassium: <3 mmol/L; >=5.5 mmol/L~Chloride: <80 mmol/L; >115 mmol/L" (NCT02373202)
Timeframe: Baseline up to Week 58

,,,
Interventionparticipants (Number)
Sodium <=129 mmol/LSodium >=160 mmol/LPotassium <3 mmol/LPotassium >=5.5 mmol/LChloride <80 mmol/LChloride >115 mmol/L
Sarilumab 150 mg q2w000000
Sarilumab 150 mg q2w + DMARDs000000
Sarilumab 200 mg q2w000000
Sarilumab 200 mg q2w + DMARDs000000

[back to top]

Number of Participants With Potentially Clinically Significant Laboratory Abnormalities: Hematological Parameters

"Criteria for potentially clinically significant abnormalities:~Hemoglobin: <=115 g/L (Male[M]) or <=95 g/L (Female[F]); >=185 g/L (M) or >=165 g/L (F); DFB >=20 g/L~Hematocrit: <=0.37 v/v (M) or <=0.32 v/v (F); >=0.55 v/v (M) or >=0.5 v/v (F)~Red blood cells (RBC): >=6 Tera/L~Platelets: <50 Giga/L; >=50 and <100 Giga/L; >=700 Giga/L~White blood cells (WBC): <3.0 Giga/L (Non-Black [NB]) or <2.0 Giga/L (Black [B]); >=16.0 Giga/L~Neutrophils: <1.5 Giga/L (NB) or <1.0 Giga/L (B); <1.0 Giga/L~Lymphocytes: <0.5 Giga/L; >=0.5 Giga/L and 4.0 Giga/L~Monocytes: >0.7 Giga/L~Basophils: >0.1 Giga/L~Eosinophils: >0.5 Giga/L or >upper limit of normal (ULN) (if ULN >=0.5 Giga/L)" (NCT02373202)
Timeframe: Baseline up to Week 58

,,,
Interventionparticipants (Number)
Hemoglobin <=115 g/L (M) or <=95 g/L (F)Hemoglobin >=185 g/L (M) or >=165 g/L (F)Hemoglobin DFB >=20 g/LHematocrit <=0.37 v/v (M) or <=0.32 v/v (F)Hematocrit >0.55 v/v (M) or >=0.5 v/v (F)RBC >=6 Tera/LPlatelets <50 Giga/LPlatelets >=50 and <100 Giga/LPlatelets >=700 Giga/LWBC <3.0 Giga/L (NB) or <2.0 Giga/L (B)WBC >=16.0 Giga/LNeutrophils <1.5 Giga/L (NB) or <1.0 Giga/L (B)Neutrophils <1.0 Giga/LLymphocytes <0.5 Giga/LLymphocytes >=0.5 Giga/L and Lymphocytes >4.0 Giga/LMonocytes >0.7 Giga/LBasophils >0.1 Giga/LEosinophils >0.5 Giga/L or >ULN (ULN >=0.5 Giga/L)
Sarilumab 150 mg q2w1002000107082030302
Sarilumab 150 mg q2w + DMARDs0000000106085030110
Sarilumab 200 mg q2w30260000090134180252
Sarilumab 200 mg q2w + DMARDs10030001090113041000

[back to top]

Number of Participants With Potentially Clinically Significant Laboratory Abnormalities: Liver Function Parameters

"Criteria for potentially clinically significant abnormalities:~Alanine Aminotransferase (ALT): >1 ULN and <=1.5 ULN; >1.5 ULN and <=3 ULN; >3 ULN and <=5 ULN; >5 ULN and <=10 ULN; >10 ULN and <=20 ULN; >20 ULN~Aspartate aminotransferase (AST): >1 ULN and <=1.5 ULN; >1.5 ULN and <=3 ULN; >3 ULN and <=5 ULN; >5 ULN and <=10 ULN; >10 ULN and <=20 ULN; >20 ULN~Alkaline phosphatase: >1.5 ULN~Total bilirubin (TBILI): >1.5 ULN; >2 ULN~Conjugated bilirubin(CBILI): >1.5 ULN~Unconjugated bilirubin: >1.5 ULN~ALT >3 ULN and TBILI >2 ULN~CBILI >35% TBILI and TBILI >1.5 ULN~Albumin: <=25 g/L" (NCT02373202)
Timeframe: Baseline up to Week 58

,,,
Interventionparticipants (Number)
ALT >1 ULN and <=1.5 ULNALT >1.5 ULN and <=3 ULNALT >3 ULN and <=5 ULNALT >5 ULN and <=10 ULNALT >10 ULN and <=20 ULNALT >20 ULNAST >1 ULN and <=1.5 ULNAST >1.5 ULN and <=3 ULNAST >3 ULN and <=5 ULNAST >5 ULN and <=10 ULNAST >10 ULN and <=20 ULNAST >20 ULNAlkaline Phosphatase >1.5 ULNTBILI >1.5 ULNTBILI >2 ULNCBILI >1.5 ULNUnconjugated Bilirubin >1.5 ULNALT> 3 ULN and TBILI >2ULNCBILI >35% TBILI and TBILI >1.5 ULNAlbumin <=25 g/L
Sarilumab 150 mg q2w73100082000000000000
Sarilumab 150 mg q2w + DMARDs32110061100001000000
Sarilumab 200 mg q2w62400043100000000000
Sarilumab 200 mg q2w + DMARDs41000050000001000000

[back to top]

Number of Participants With Potentially Clinically Significant Laboratory Abnormalities: Metabolic Parameters

"Criteria for potentially clinically significant abnormalities:~Glucose: <=3.9 mmol/L and =11.1 mmol/L (unfasted [unfas]) or >=7 mmol/L (fasted [fas])~Hemoglobin A1c (HbA1c): >8%~Total cholesterol: >=6.2 mmol/L; >=7.74 mmol/L~LDL cholesterol: >=4.1 mmol/L; >=4.9 mmol/L~Triglycerides: >=4.6 mmol/L; >=5.6 mmol/L" (NCT02373202)
Timeframe: Baseline up to Week 58

,,,
Interventionparticipants (Number)
Glucose <=3.9 mmol/L and Glucose >=11.1 mmol/L (unfas) or >=7 mmol/L (fas)HbA1c >8%Total Cholesterol >=6.2 mmol/LTotal Cholesterol >=7.74 mmol/LLDL Cholesterol >=4.1 mmol/LLDL Cholesterol >=4.9 mmol/LTriglycerides >=4.6 mmol/LTriglycerides >=5.6 mmol/L
Sarilumab 150 mg q2w1001216200
Sarilumab 150 mg q2w + DMARDs000611000
Sarilumab 200 mg q2w1211323111
Sarilumab 200 mg q2w + DMARDs010713100

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Number of Participants With Potentially Clinically Significant Laboratory Abnormalities: Renal Function Parameters

"Criteria for potentially clinically significant abnormalities:~Creatinine: >=150 micromol/L (adults); >=30% change from baseline, >=100% change from baseline~Creatinine clearance: <15 mL/min; >=15 to <30 mL/min; >=30 to <60 mL/min; >=60 to <90 mL/min~Blood urea nitrogen: >=17 mmol/L~Uric acid: <120 micromol/L; >408 micromol/L" (NCT02373202)
Timeframe: Baseline up to Week 58

,,,
Interventionparticipants (Number)
Creatinine >=150 micromol/L (Adults)Creatinine >=30% change from baselineCreatinine >=100% change from baselineCreatinine Clearance <15 mL/minCreatinine clearance >=15 to <30 mL/minCreatinine clearance >=30 to <60 mL/minCreatinine clearance >=60 to <90 mL/minBlood Urea Nitrogen >=17 mmol/LUric acid <120 micromol/LUric acid >408 micromol/L
Sarilumab 150 mg q2w06000615002
Sarilumab 150 mg q2w + DMARDs0300068001
Sarilumab 200 mg q2w15000517004
Sarilumab 200 mg q2w + DMARDs0300067011

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Number of Participants With Potentially Clinically Significant Vital Signs Abnormalities

"Criteria for potentially clinically significant vital sign abnormalities:~Systolic blood pressure (SBP) supine: <=95 mmHg and decrease from baseline (DFB) >=20 mmHg; >=160 mmHg and increase from baseline (IFB) >=20 mmHg~Diastolic blood pressure (DBP) supine: <=45 mmHg and DFB >=10 mmHg; >=110 mmHg and IFB ≥10 mmHg~SBP (Orthostatic): <=-20 mmHg~DBP (Orthostatic): <=-10 mmHg~Heart rate (HR) supine: <=50 beats per minute (bpm) and DFB >=20 bpm; >=120 bpm and IFB >=20 bpm~Weight: >=5% DFB; >=5% IFB" (NCT02373202)
Timeframe: Baseline up to Week 58

,,,
Interventionparticipants (Number)
SBP (supine) <=95 mmHg and DFB >=20 mmHgSBP (supine) >=160 mmHg and IFB >=20 mmHgDBP (supine) <=45 mmHg and DFB >=10 mmHgDBP (supine) >=110 mmHg and IFB >=10 mmHgSBP (orthostatic) <=-20 mmHgDBP (orthostatic) <=-10 mmHgHR (supine) <=50 bpm and DFB >= 20 bpmHR (supine) >=120 bpm and IFB >=20 bpmWeight >=5% DFBWeight >=5% IFB
Sarilumab 150 mg q2w01005510212
Sarilumab 150 mg q2w + DMARDs0100830013
Sarilumab 200 mg q2w01009101007
Sarilumab 200 mg q2w + DMARDs0100530012

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Number of Participants With Treatment-Emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)

Adverse event (AE) was defined as any untoward medical occurrence in a participant who received IMP and did not necessary have to had a causal relationship with treatment. All AEs that occurred from the first dose of the IMP administration up to 6 weeks after last dose of treatment (up to Week 58) were considered as TEAEs. SAEs were AEs resulting in any of the following outcomes or deemed significant for any other reason: death; initial or prolonged inpatient hospitalization; life-threatening experience (immediate risk of dying); persistent or significant disability/incapacity; congenital anomaly or a medically important event. TEAEs included both SAEs and non-SAEs. (NCT02373202)
Timeframe: Baseline up to Week 58

,,,
Interventionparticipants (Number)
Any TEAESAE
Sarilumab 150 mg q2w251
Sarilumab 150 mg q2w + DMARDs140
Sarilumab 200 mg q2w282
Sarilumab 200 mg q2w + DMARDs133

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Percentage of Participants Achieving American College of Rheumatology (ACR) 20, 50 and 70 Responses at Week 52

ACR response is a composite rating scale that includes 7 variables: tender joints count (TJC [68 joints]); swollen joints count (SJC [66 joints]); levels of an acute phase reactant (high sensitivity C-reactive protein [hs-CRP level]); participant's assessment of pain (measured on 0 [no pain]-100 mm [worst pain] visual analog scale [VAS]); participant's global assessment of disease activity (measured on 0 [no arthritis activity]-100 mm [maximal arthritis activity] VAS); physician's global assessment of disease activity (measured on 0 [no arthritis activity]-100 mm [maximal arthritis activity] VAS); participant's assessment of physical function (measured by Health Assessment Question-Disability Index [HAQ-DI], with scoring range of 0 [better health] - 3 [worst health]). ACR20/50/70 response is defined as at least 20/50/70% improvement in both TJC and SJC, and at least 20/50/70% improvement in at least 3 of the 5 other assessments, respectively. (NCT02373202)
Timeframe: Week 52

,,,
Interventionpercentage of participants (Number)
ACR20ACR50ACR70
Sarilumab 150 mg q2w76.756.726.7
Sarilumab 150 mg q2w + DMARDs73.360.053.3
Sarilumab 200 mg q2w74.254.825.8
Sarilumab 200 mg q2w + DMARDs40.033.326.7

[back to top]