cyclosporin G: similar immunosuppressive actions as cyclosporin, but without nephrotoxic side effects; cyclosporin A analog; MW 1217 [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 6475296 |
| CHEMBL ID | 2107422 |
| SCHEMBL ID | 2110698 |
| MeSH ID | M0132448 |
| Synonym |
|---|
| cyclosporin g |
| (3s,6s,9s,12r,15s,18s,21s,24s,30s,33s)-33-[(e,1r,2r)-1-hydroxy-2-methyl-hex-4-enyl]-6,9,18,24-tetraisobutyl-3,21-diisopropyl-1,4,7,10,12,15,19,25,28-nonamethyl-30-propyl-1,4,7,10,13,16,19,22,25,28,31-undecazacyclotritriacontane-2,5,8,11,14,17,20,23,26,29, |
| 74436-00-3 |
| geclosporin |
| cyclosporin a, 7-l-norvaline- |
| cyclosporine g |
| geclosporin [inn] |
| cyclo(((2s,3r,4r,6e)-3-hydroxy-4-methyl-2-(methylamino)-6-octenoyl)-l-norvalyl-n-methylglycyl-n-methyl-l-leucyl-l-valyl-n-methyl-l-leucyl-l-alanyl-d-alanyl-n-methyl-l-leucyl-n-methyl-l-leucyl-n-methyl-l-valyl) |
| (3s,6s,9s,12r,15s,18s,21s,24s,30s,33s)-33-[(e,1r,2r)-1-hydroxy-2-methylhex-4-enyl]-1,4,7,10,12,15,19,25,28-nonamethyl-6,9,18,24-tetrakis(2-methylpropyl)-3,21-di(propan-2-yl)-30-propyl-1,4,7,10,13,16,19,22,25,28,31-undecazacyclotritriacontane-2,5,8,11,14,1 |
| og-37-325 |
| sdz-37-325 |
| CHEMBL2107422 |
| cyclosporin-g |
| unii-ua3jnw70t9 |
| ua3jnw70t9 , |
| bdbm50422041 |
| cyclosporin g [mi] |
| cyclo((2s,3r,4r,6e)-3-hydroxy-4-methyl-2-(methylamino)-6-octenoyl-l-norvalyl-n-methylglycyl-n-methyl-l-leucyl-l-valyl-n-methyl-l-leucyl-l-alanyl-d-alanyl-n-methyl-l-leucyl-n-methyl-l-leucyl-n-methyl-l-valyl) |
| cyclo(l-alanyl-d-alanyl-n-methyl-l-leucyl-n-methyl-l-leucyl-n-methyl-l-valyl-(3r,4r,6e)-6,7-didehydro-3-hydroxy-n,4-dimethyl-l-2-aminooctanoyl-l-norvalyl-n-methylglycyl-n-methyl-l-leucyl-l-valyl-n-methyl-l-leucyl) |
| SCHEMBL2110698 |
| EX-A2493 |
| Q27290967 |
| 4-(5-formyl-thiazol-2-yl)-piperazine-1-carboxylicacidtert-butylester |
| BC171087 |
Cyclosporin G is a new immunosuppressor structurally similar to cyclospor in A.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Cyclosporin G (CsG) is an analogue of cyclosporin A (CsA) with strong immunosuppressive activity. " | ( Experimental nephrotoxicity, hepatotoxicity and pharmacokinetics of cyclosporin G versus cyclosporin A. Andoh, TF; Bennett, WM; Burdmann, EA; Elzinga, LW; Lindsley, J; Munar, MY; Rosen, S, 1994) | 1.97 |
| "Cyclosporin G is a new immunosuppressor structurally similar to cyclosporin A. " | ( Metabolism of the new immunosuppressor cyclosporin G by human liver cytochromes P450. Domergue, J; Fourtanier, G; Koch, P; Maurel, P; Pichard, L; Schran, HF, 1996) | 2.01 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "Cyclosporin G (CSG) has produced less nephrotoxicity than cyclosporin A (CSA) at equivalent doses in animal models. " | ( Comparative pharmacokinetics and renal effects of cyclosporin A and cyclosporin G in renal allograft recipients. Conti, DJ; Drusano, G; Gallichio, M; Gruber, SA; Hughes, SE; Kaplan, SS; Lempert, N; Rosano, TG; Singh, TP; Stein, DS; Urbauer, DL, 1997) | 1.98 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " FK506 metabolites exhibit greater toxicity than the parent drug, while CsA metabolites are far less toxic than CsA itself." | ( Implication of CYP 3A in the toxicity of cyclosporin G (CsG), cyclosporin A (CsA) and FK506 on rat hepatocytes in primary culture. Claude, JR; Duc, HT; Dutertre-Catella, H; Ellouk-Achard, S; Martin, C; Pham-Huy, C; Thevenin, M; Warnet, JM, 1997) | 0.56 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " The resulting pharmacokinetic parameters of CsG were similar to those described for CsA in the same patient population." | ( Pharmacokinetics of cyclosporine G in patients with renal failure. Abisch, E; Beveridge, T; Bindschedler, M; Costa, E; Follath, F; Keller, HP; Thiel, G; Vozeh, S; Wenk, M; Zuber, M, 1988) | 0.27 |
| "This study examined the effects of the widely used immunosuppressor cyclosporine A and of one of its derivatives, cyclosporine G, on glucose tolerance, cellular immunity, and renal and hepatic function, in relation to their pharmacokinetic profile in Wistar rats." | ( Pharmacokinetic profile of cyclosporine A and G and their effects on cellular immunity and glucose tolerance in male and female Wistar rats. Faraci, M; Vigeant, C; Yale, JF, 1988) | 0.27 |
| " In blood, the terminal half-life of CsG and total radioactivity averaged 9-11 hr following both the 150 and 600 mg doses." | ( Pharmacokinetics and metabolism of cyclosporin G in humans. Mangold, JB; Schran, HF; Tse, FL, ) | 0.41 |
| "New approaches for empirical and model-based development of constrained, limited sampling strategies for the estimation of one or more characteristics of a pharmacokinetic (PK) profile are evaluated." | ( Development of limited sampling strategies for characteristics of a pharmacokinetic profile. Sallas, WM, 1995) | 0.29 |
| " The objective of the study was to examine steady-state pharmacokinetic profiles of adult renal allograft recipients receiving CSA and CSG in relation to concentrations of endothelin-1 and NO2/NO3 in urine and plasma, creatinine clearance (Clcr), and urinary excretion of N-acetyl-beta-D-glucosaminidase (NAG) 9 months after transplantation." | ( Comparative pharmacokinetics and renal effects of cyclosporin A and cyclosporin G in renal allograft recipients. Conti, DJ; Drusano, G; Gallichio, M; Gruber, SA; Hughes, SE; Kaplan, SS; Lempert, N; Rosano, TG; Singh, TP; Stein, DS; Urbauer, DL, 1997) | 0.53 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "5 and 3 hr, and the bioavailability was in the range of 24-55% (mean 36%)." | ( Pharmacokinetics of cyclosporine G in patients with renal failure. Abisch, E; Beveridge, T; Bindschedler, M; Costa, E; Follath, F; Keller, HP; Thiel, G; Vozeh, S; Wenk, M; Zuber, M, 1988) | 0.27 |
| "A concentration-guided study was designed to maintain adequate immunosuppression and avoid excessive drug exposure while determining steady-state relative bioavailability of two cyclosporine G (CyG) oral formulations in stable renal transplant patients." | ( Concentration-guided strategies in drug development: experience with a cyclosporine analog in transplantation. Arns, W; Kallay, Z; Kovarik, JM; Lison, AE; Mueller, EA; Renner, E; Smith, HT, 1995) | 0.29 |
| Excerpt | Relevance | Reference |
|---|---|---|
| " Evaluation of the immunosuppressive efficacy and assessment of possible side effects of CsG was made and compared with the results in 38 historical control patients starting with the same dose of CsA as part of the same immunosuppressive dosage schedule." | ( The efficacy and tolerability of cyclosporine G in human kidney transplant recipients. Beveridge, T; Bianchi, L; Huser, B; Landmann, J; Mihatsch, MJ; Oberholzer, M; Thiel, G, 1992) | 0.28 |
| " Addition of exogenous lymphokines in the form of rat spleen concanavalin A (Con A)-conditioned medium (SCM) or recombinant IL-2 (but not recombinant IL-1) was able to reverse only about half of the inhibition, as measured along the linear part of the dose-response curve." | ( Differential effects of cyclosporins A and G on functional activation of a T-helper-lymphocyte line mediating experimental autoimmune uveoretinitis. Caspi, RR; Gery, I; McAllister, CG; Nussenblatt, RB, 1988) | 0.27 |
| " All animals received a small dosage of steroids (0." | ( Comparative effect of cyclosporin A and G on weight gain of primates during the pubertal growth period. Baldwin, JC; Billingham, ME; Harjula, A; Hoffman, AR; Shumway, NE, ) | 0.13 |
| " When stable dosing was achieved, there was a measured 6-fold variation in the ratio of 12-hr whole-blood parent compound trough concentration (ng/ml, HPLC) to daily OG 37-325 dose (mg/kg) ([OG 37-325]/dose)." | ( Prediction of interpatient and intrapatient variation in OG 37-325 dosing requirements by the erythromycin breath test. A prospective study in renal transplant recipients. Annesley, TM; Blake, DS; Leichtman, AB; Lown, KS; Schmouder, RL; Turgeon, DK; Watkins, PB, 1994) | 0.29 |
| "The steady-state concentrations of cyclosporin G (OG37-325) (CsG) and six of its metabolites (GM1, GM9, GM4N, GM1c, GM1c9, GM19) were measured throughout the 12-h dosing interval in six renal transplant recipients receiving CsG as prophylaxis against acute cellular rejection." | ( Steady-state concentration of cyclosporin G (OG37-325) and its metabolites in renal transplant recipients. Langman, LJ; Leichtman, AB; Weitzel, WF; Yatscoff, RW, 1994) | 0.85 |
| " When both drugs were given in the same dosage on a weight basis (15 mg/kg/day, subcutaneously), CsA blood levels were higher than CsG (3305 vs." | ( Experimental nephrotoxicity, hepatotoxicity and pharmacokinetics of cyclosporin G versus cyclosporin A. Andoh, TF; Bennett, WM; Burdmann, EA; Elzinga, LW; Lindsley, J; Munar, MY; Rosen, S, 1994) | 0.52 |
| " CsG has immunosuppressive effects equivalent to CsA when dosed on a weight basis." | ( Production of less chronic nephrotoxicity by cyclosporine G than cyclosporine A in a low-salt rat model. Andoh, T; Bennett, WM; Burdmann, EA; Elzinga, L; Lindsley, J; Rosen, S, 1993) | 0.29 |
| " Patient groups were defined as follows: group 1: initial CSA (n = 6); group 2: initial CSG (n = 7); group 3: five of the seven patients in group 2 taking CSG subsequently undergoing conversion to CSA; group 4: the same five patients in group 3 restudied 1 month after 1:1 dosage conversion to CSA; and group 5: CSA groups 1 and 4 combined (n = 11)." | ( Comparative pharmacokinetics and renal effects of cyclosporin A and cyclosporin G in renal allograft recipients. Conti, DJ; Drusano, G; Gallichio, M; Gruber, SA; Hughes, SE; Kaplan, SS; Lempert, N; Rosano, TG; Singh, TP; Stein, DS; Urbauer, DL, 1997) | 0.53 |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Interleukin-2 | Mus musculus (house mouse) | IC50 (µMol) | 0.0130 | 0.0050 | 0.0090 | 0.0130 | AID91889 |
| Peptidyl-prolyl cis-trans isomerase A | Homo sapiens (human) | IC50 (µMol) | 0.2200 | 0.0020 | 0.1438 | 1.5490 | AID54724; AID54725 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| RNA binding | Peptidyl-prolyl cis-trans isomerase A | Homo sapiens (human) |
| peptidyl-prolyl cis-trans isomerase activity | Peptidyl-prolyl cis-trans isomerase A | Homo sapiens (human) |
| integrin binding | Peptidyl-prolyl cis-trans isomerase A | Homo sapiens (human) |
| protein binding | Peptidyl-prolyl cis-trans isomerase A | Homo sapiens (human) |
| cyclosporin A binding | Peptidyl-prolyl cis-trans isomerase A | Homo sapiens (human) |
| virion binding | Peptidyl-prolyl cis-trans isomerase A | Homo sapiens (human) |
| unfolded protein binding | Peptidyl-prolyl cis-trans isomerase A | Homo sapiens (human) |
| heparan sulfate binding | Peptidyl-prolyl cis-trans isomerase A | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 38 (34.86) | 18.7374 |
| 1990's | 67 (61.47) | 18.2507 |
| 2000's | 2 (1.83) | 29.6817 |
| 2010's | 0 (0.00) | 24.3611 |
| 2020's | 2 (1.83) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.
| This Compound (25.67) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 12 (10.53%) | 5.53% |
| Reviews | 6 (5.26%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 96 (84.21%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||