5-HT2A receptor antagonists(Serotonin 2a (5-HT2a) receptor antagonists), D1 receptor antagonists(Dopamine D1 receptor antagonists), D2 receptor antagonists(Dopamine D2 receptor antagonists)

Therapeutic Areas

Other Diseases

Active Indication-

Inactive Indication

Schizophrenia

Originator Organization

Pfizer Inc.

Active Organization-

Inactive Organization

Pfizer Inc.

Drug Highest PhaseWithdrawn

First Approval Date

United States (06 Apr 1970),

Schizophrenia

Regulation-

Structure/Sequence

Molecular FormulaC23H35Cl2N3O4S2

InChIKeyMEUAAEMCZUPORO-LRSHZYOCSA-N

CAS Registry22189-31-7

View All Structures (2)

100 Clinical Results associated with Thiothixene Hydrochloride

100 Translational Medicine associated with Thiothixene Hydrochloride

100 Patents (Medical) associated with Thiothixene Hydrochloride

245

Literatures (Medical) associated with Thiothixene Hydrochloride

01 Jul 2015·Journal of Pharmaceutical and Biomedical Analysis

Method development for impurity profiling in SFC: The selection of a dissimilar set of stationary phases

Article

Author: Heyden, Yvan Vander ; Galea, Charlene ; Mangelings, Debby

Supercritical fluid chromatography (SFC) is drawing considerable interest as separation technique in the pharmaceutical industry. The technique is already well established in chiral separations both analytically and on a preparative scale. The use of SFC as a technique for drug impurity profiling is examined here. To define starting conditions in method development for drug impurity profiling, a set of dissimilar stationary phases is screened in parallel. The possibility to select a set of dissimilar columns using the retention factors (k-values) for a set of 64 drugs measured on 27 columns in SFC was examined. Experiments were carried out at a back-pressure of 150 bar and 25 °C with a mobile phase consisting of CO2 and methanol with 0.1% isopropylamine (5-40% over 10 min) at a flow rate of 3 mL/min. These k-values were then used to calculate correlation coefficients on the one hand and to perform a principal component analysis on the other. The Kennard and Stone algorithm, besides dendrograms and correlation-coefficient colour maps were used to select a set of 6 dissimilar stationary phases. The stationary phase characterization results from this study were compared to those from previous studies found in the literature. Retention mechanisms for compounds possessing different properties were also evaluated. The dissimilarity of the selected subset of 6 stationary phases was validated using mixtures of compounds with similar properties and structures, as one can expect in a drug impurity profile.

01 Feb 2015·Journal of Clinical PsychopharmacologyQ4 · MEDICINE

Weight Gain on Antipsychotic Medication Is Associated With Sustained Use Among Veterans With Schizophrenia

Q4 · MEDICINE

Article

Author: Lawler, Elizabeth V. ; Chittamooru, Subha ; Monnelly, Edward P. ; Gagnon, David R. ; Fonda, Jennifer

OBJECTIVEContinuous antipsychotic treatment is important in schizophrenia, and studies have shown that rates of discontinuation are high. Some studies suggest that weight gain may lead schizophrenic patients to discontinue treatment, whereas other studies show smaller effects of weight gain on medication discontinuation, and some find weight gain associated with symptom improvement. Our retrospective cohort study investigated the effect of weight change on the continued use for 1 year (persistence) of all antipsychotics, then among users of first-generation antipsychotics and second-generation antipsychotics (SGAs), and lastly subgroups of SGAs.METHODSWe identified 2130 patients with schizophrenia starting an antipsychotic that had not used 1 in the prior year. Using multivariable logistic regression adjusted for demographic and clinical variables, we determined the odds of remaining persistent on medication among patients who either gained weight or did not gain weight in the following year.RESULTSFor all antipsychotics combined, weight change was not associated with persistence. Among SGAs, weight gain was associated with a 23% increase in the adjusted odds ratio (OR) for persistence (OR, 1.23; 95% confidence interval [CI], 1.00-1.51), whereas there was a nonsignificant decrease in the adjusted odds of persistence among first-generation antipsychotic users (OR, 0.74; 95% CI, 0.43-1.28). When SGAs were divided into subgroups (clozapine/olanzapine, risperidone/quetiapine), both had increases in the likelihood of persistence, but only the association for clozapine/olanzapine was significant at a trend level (adjusted OR, 1.46; 95% CI, 0.99-2.16).CONCLUSIONSThese findings are supportive of other research that shows weight gain does not invariably lead to medication discontinuation and may be associated with clinical improvement.

01 Jan 2015·European Journal of Pharmaceutical SciencesQ2 · MEDICINE

Quantitative NTCP pharmacophore and lack of association between DILI and NTCP Inhibition

Q2 · MEDICINE

Article

Author: Ekins, Sean ; Polli, James E ; Dong, Zhongqi

The human sodium taurocholate cotransporting polypeptide (NTCP) is a hepatic bile acid transporter. Inhibition of NTCP uptake may potentially also prevent hepatitis B virus (HBV) infection. The first objective was to develop a quantitative pharmacophore for NTCP inhibition. Recent studies showed that hepatotoxic drugs could inhibit bile acid uptake into hepatocytes, without inhibiting canalicular efflux, and cause bile acid elevation in plasma. Hence, a second objective was to examine whether NTCP inhibition is associated with drug induced liver injury (DILI). Twenty-seven drugs from our previous study were used as the training set to develop a quantitative pharmacophore. From secondary screening from a drug database, six retrieved drugs and three drugs not retrieved by the model were tested for NTCP inhibition. Tertiary screening involved drugs known to cause DILI and not cause DILI. Overall, ninety-four drugs were assessed for hepatotoxicity and were assessed relative to NTCP inhibition. The quantitative pharmacophore possessed one hydrogen bond acceptor, one hydrogen bond donor, a hydrophobic feature, and excluded volumes. From 94 drugs, NTCP inhibitors and non-inhibitors were approximately equally distributed across the drugs of most DILI concern, less DILI concern, and no DILI concern, indicating no relationship between NTCP inhibition and DILI risk. Hence, an approach to treat HBV via NTCP inhibition is not expected to be associated with DILI.

100 Deals associated with Thiothixene Hydrochloride

External Link

KEGG	Wiki	ATC	Drug Bank
D02612	Thiothixene Hydrochloride	N05AF04	DBSALT001423

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