Tesofensine: an appetite suppressant [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 11370864 |
| CHEMBL ID | 3989690 |
| SCHEMBL ID | 37509 |
| MeSH ID | M0508296 |
| Synonym |
|---|
| ns-2330 |
| tesofensine |
| 195875-84-4 |
| (1r-(2-endo,3-exo))-3-(3,4-dichlorophenyl)-2-(ethoxymethyl)-8-methyl-8-azabicyclo(3,2,1)octane-2-hydroxy-1,2,3-propanetricarboxylate |
| ns 2330 |
| tesofensine [inn] |
| 8-azabicyclo(3.2.1)octane, 3-(3,4-dichlorophenyl)-2-(ethoxymethyl)-8-methyl-, (1r-(2-endo,3-exo))- |
| unii-blh9ukx9v1 |
| blh9ukx9v1 , |
| (1r,2r,3s,5s)-3-(3,4-dichlorophenyl)-2-(ethoxymethyl)-8-methyl-8-azabicyclo(3.2.1)octane |
| ns2330 |
| tesofensine [who-dd] |
| tesofensine [mi] |
| tesofensine [mart.] |
| SCHEMBL37509 |
| (1r,2r,3s)-2-ethoxymethyl-3-(3,4-dichlorophenyl)tropane |
| VCVWXKKWDOJNIT-ZOMKSWQUSA-N |
| (1r, 2r, 3s)-2-ethoxymethyl-3-(3,4-dichlorophenyl)tropane |
| (1r,2r,3s,5s)-3-(3,4-dichlorophenyl)-2-(ethoxymethyl)-8-methyl-8-azabicyclo[3.2.1]octane |
| AKOS027326890 |
| J-012675 |
| CHEMBL3989690 |
| DTXSID70905114 |
| DB06156 |
| Q7705544 |
| MS-24909 |
| HY-14472 |
| CS-0003378 |
Tesofensine (TE) is a new drug producing twice the weight loss in obese individuals as seen with currently marketed drugs. It inhibits both norepinephrine, 5-HT, and dopamine (DA) reuptake function.
Tesofensine treatment (2.0 mg/kg/day for 14 days) caused a pronounced anorexigenic and weight-reducing response in DIO rats as compared to age-matched chow-fed rats. Tesofensin-treated rats showed significantly lower D2/3R availability in nucleus accumbens and dorsal striatum.
The aims of this investigation were to simultaneously accomplish a thorough characterization of the pharmacokinetic (PK) properties of tesofensine and M1 in mice. The inhibition of the dopamine transporter was determined by co-administration of [(3)H]WIN35,428 as the pharmacodynamic measure.
| Excerpt | Reference | Relevance |
|---|---|---|
| "To develop a population pharmacokinetic model for NS2330 and its major metabolite M1 based on data from a 14 week proof of concept study in patients with Alzheimer's disease, and to identify covariates that might influence the pharmacokinetic characteristics of the drug and/or its metabolite." | ( Population pharmacokinetic modelling of NS2330 (tesofensine) and its major metabolite in patients with Alzheimer's disease. Kloft, C; Lehr, T; Raschig, A; Schaefer, HG; Staab, A; Tillmann, C; Trommeshauser, D, 2007) | 0.6 |
| " The aims of this investigation were (i) to simultaneously accomplish a thorough characterization of the pharmacokinetic (PK) properties of tesofensine and M1 in mice and (ii) to evaluate the potency (pharmacodynamics, PD) and concentration-time course of the active metabolite M1 relative to tesofensine and their impact in vivo using the PK/PD modelling approach." | ( Contribution of the active metabolite M1 to the pharmacological activity of tesofensine in vivo: a pharmacokinetic-pharmacodynamic modelling approach. Kloft, C; Lehr, T; Nielsen, EØ; Schaefer, HG; Staab, A; Tillmann, C; Trommeshauser, D, 2008) | 0.78 |
| " Concentrations of tesofensine and M1 were measured; inhibition of the dopamine transporter was determined by co-administration of [(3)H]WIN35,428 as the pharmacodynamic measure." | ( Contribution of the active metabolite M1 to the pharmacological activity of tesofensine in vivo: a pharmacokinetic-pharmacodynamic modelling approach. Kloft, C; Lehr, T; Nielsen, EØ; Schaefer, HG; Staab, A; Tillmann, C; Trommeshauser, D, 2008) | 0.9 |
| " The most appropriate method for data analysis might be a semi-mechanistic population pharmacokinetic modelling approach." | ( Semi-mechanistic population pharmacokinetic drug-drug interaction modelling of a long half-life substrate and itraconazole. Kloft, C; Lehr, T; Schaefer, HG; Staab, A; Trommeshauser, D, 2010) | 0.36 |
| " First, pharmacokinetic models of itraconazole and tesofensine were developed in parallel." | ( Semi-mechanistic population pharmacokinetic drug-drug interaction modelling of a long half-life substrate and itraconazole. Kloft, C; Lehr, T; Schaefer, HG; Staab, A; Trommeshauser, D, 2010) | 0.61 |
| "This analysis presents a semi-mechanistic population pharmacokinetic approach that may be useful for the evaluation of DDI studies." | ( Semi-mechanistic population pharmacokinetic drug-drug interaction modelling of a long half-life substrate and itraconazole. Kloft, C; Lehr, T; Schaefer, HG; Staab, A; Trommeshauser, D, 2010) | 0.36 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "For compounds with a long elimination half-life, the evaluation of a drug-drug interaction (DDI) study can be challenging." | ( Semi-mechanistic population pharmacokinetic drug-drug interaction modelling of a long half-life substrate and itraconazole. Kloft, C; Lehr, T; Schaefer, HG; Staab, A; Trommeshauser, D, 2010) | 0.36 |
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 15 (51.72) | 29.6817 |
| 2010's | 14 (48.28) | 24.3611 |
| 2020's | 0 (0.00) | 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 very strong demand-to-supply ratio for research on this compound.
| This Compound (69.33) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 10 (34.48%) | 5.53% |
| Reviews | 4 (13.79%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 15 (51.72%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||