ID Source | ID |
---|---|
PubMed CID | 49831411 |
CHEMBL ID | 2219425 |
CHEBI ID | 90930 |
SCHEMBL ID | 1044330 |
MeSH ID | M000613234 |
Synonym |
---|
alks-9070 |
alks-9072 |
aristada initio |
rdc3317 |
CHEMBL2219425 |
rdc 3317 |
alks 9070 |
1259305-29-7 |
b786j7a343 , |
unii-b786j7a343 |
aripiprazole lauroxil , |
dodecanoic acid, (7-(4-(4-(2,3-dichlorophenyl)-1-piperazinyl)butoxy)-3,4-dihydro-2-oxo-1(2h)-quinolinyl)methyl ester |
alks 9072 |
(7-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butoxy)-2-oxo-3,4-dihydroquinolin-1(2h)-yl)methyl dodecanoate |
aristada |
aripiprazole lauroxil [usan] |
rdc-3317 |
aripiprazole lauroxil (usan) |
D10364 |
aristada (tn) |
SCHEMBL1044330 |
aripiprazole lauroxil [mi] |
aripiprazole lauroxil [who-dd] |
aripiprazole lauroxil [orange book] |
CHEBI:90930 , |
[7-{4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butoxy}-2-oxo-3,4-dihydroquinolin-1(2h)-yl]methyl dodecanoate |
[7-[4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butoxy]-2-oxo-3,4-dihydroquinolin-1-yl]methyl dodecanoate |
DTXSID60154997 , |
dodecanoic acid [7-[4-[4-(2,3-dichlorophenyl)-1-piperazinyl]butoxy]-3,4-dihydro-2-oxo-1(2h)-quinolinyl]methyl ester |
mfcd26967976 |
AKOS030627657 |
aripiprazol- lauroxil |
DB14185 |
AS-35241 |
Q25323757 |
EX-A4069 |
BCP14993 |
aripiprazole-lauroxil |
HY-108751 |
CS-0030962 |
NCGC00532501-01 |
A856290 |
dtxcid5077488 |
aristada initio kit |
dodecanoic acid, [7-[4-[4-(2,3-dichlorophenyl)-1-piperazinyl]butoxy]-3,4-dihydro-2-oxo-1(2h)-quinolinyl]methyl ester |
(7-{4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butoxy}-2-oxo-1,2,3,4-tetrahydroquinolin-1-yl)methyl dodecanoate |
EN300-7416466 |
AC-36504 |
Aripiprazole lauroxil (AL) is a long-acting atypical antipsychotic approved for the treatment of schizophrenia in adults. It is an extended-release prodrug of aripipazole for intramuscular injection, approved for schizophrenia treatment.
Excerpt | Reference | Relevance |
---|---|---|
"Treatment with aripiprazole lauroxil resulted in decreases in agitation and hostility in patients with schizophrenia and this antihostility effect appears to be independent of a general antipsychotic effect." | ( Effect of aripiprazole lauroxil on agitation and hostility in patients with schizophrenia. Bose, A; Citrome, L; Claxton, A; Du, Y; Ehrich, EW; Risinger, R; Silverman, BL; Stankovic, S; Zummo, J, 2016) | 1.18 |
A dosing interval of 882 mg every 6 weeks results in concentrations that fall within the concentration range associated with the efficacious aripiprazole lauroxil dose range (441-882 mg dosed monthly) We developed a population pharmacokinetic (PopPK) model to evaluate dosing scenarios likely to be encountered in clinical practice.
Excerpt | Relevance | Reference |
---|---|---|
" The pharmacokinetic profile of AL also led to approval of dosing intervals of every 6 weeks for the 882 mg dose." | ( Aripiprazole long-acting injectable formulations for schizophrenia: aripiprazole monohydrate and aripiprazole lauroxil. Citrome, L, 2016) | 0.65 |
" We developed a population pharmacokinetic (PopPK) model to characterize aripiprazole lauroxil PK and evaluate dosing scenarios likely to be encountered in clinical practice." | ( Aripiprazole Lauroxil: Pharmacokinetic Profile of This Long-Acting Injectable Antipsychotic in Persons With Schizophrenia. Citrome, L; Hard, ML; Mills, RJ; Sadler, BM; Turncliff, RZ, 2017) | 2.13 |
" The model was subsequently used to evaluate various dose levels and frequency and the impact of dosing delay on aripiprazole concentrations." | ( Aripiprazole Lauroxil: Pharmacokinetic Profile of This Long-Acting Injectable Antipsychotic in Persons With Schizophrenia. Citrome, L; Hard, ML; Mills, RJ; Sadler, BM; Turncliff, RZ, 2017) | 1.9 |
" Based on the PopPK model simulations, a dosing interval of 882 mg every 6 weeks results in aripiprazole concentrations that fall within the concentration range associated with the efficacious aripiprazole lauroxil dose range (441-882 mg dosed monthly)." | ( Aripiprazole Lauroxil: Pharmacokinetic Profile of This Long-Acting Injectable Antipsychotic in Persons With Schizophrenia. Citrome, L; Hard, ML; Mills, RJ; Sadler, BM; Turncliff, RZ, 2017) | 2.09 |
"This PopPK model and model-based simulations were effective means for evaluating aripiprazole lauroxil dosing regimens and management of missed doses." | ( Aripiprazole Lauroxil: Pharmacokinetic Profile of This Long-Acting Injectable Antipsychotic in Persons With Schizophrenia. Citrome, L; Hard, ML; Mills, RJ; Sadler, BM; Turncliff, RZ, 2017) | 2.12 |
"We examined the feasibility of a 2-month (every 8 weeks [q8wk]) dosing interval of AL in a phase I open-label pharmacokinetic study investigating AL 1064 mg administered q8wk for 24 weeks, followed by 20 weeks of safety and pharmacokinetic measurements (ClinicalTrials." | ( Pharmacokinetic Profile of a 2-Month Dose Regimen of Aripiprazole Lauroxil: A Phase I Study and a Population Pharmacokinetic Model. Hard, ML; Mills, RJ; Sadler, BM; von Moltke, L; Wehr, AY; Weiden, PJ, 2017) | 0.7 |
" Study limitations included use of a fixed dose for initial oral aripiprazole and fixed monthly AL doses without the option to individualize the oral initiation dosing or injection frequency for efficacy, tolerability, or safety." | ( Effect of aripiprazole lauroxil in patients with acute schizophrenia as assessed by the Positive and Negative Syndrome Scale-supportive analyses from a Phase 3 study. Citrome, L; Cutler, AJ; Du, Y; Nasrallah, HA; Risinger, R; Silverman, BL; Zummo, J, 2018) | 0.88 |
" The PK results from this study show that a dosing interval of every 8 weeks for the 1064 mg dose resulted in aripiprazole concentrations within the established therapeutic window for AL." | ( A Phase-1 Study Comparing Pharmacokinetic and Safety Profiles of Three Different Dose Intervals of Aripiprazole Lauroxil. Hard, M; Risinger, R; Weiden, PJ, 2017) | 0.67 |
"Concomitant administration of the 1-day initiation regimen with all approved AL dosing regimens (441, 662, or 882 mg monthly, 882 mg every 6 weeks, or 1064 mg every 2 months) is predicted to achieve aripiprazole concentrations associated with therapeutic doses of AL using the 21-day initiation regimen within 4 days, maintaining these concentrations until the next AL dose." | ( Population Pharmacokinetic Analysis and Model-Based Simulations of Aripiprazole for a 1-Day Initiation Regimen for the Long-Acting Antipsychotic Aripiprazole Lauroxil. Hard, ML; Mills, RJ; Sadler, BM; von Moltke, L; Wehr, AY, 2018) | 0.68 |
" Long-acting injectable (LAI) antipsychotics offer an extended dosing interval option for patients, although the current options may require an oral overlap at initiation." | ( Aripiprazole Lauroxil NanoCrystal Clark, C; Davis, E; Ehret, MJ; Luttrell, SE, ) | 1.57 |
"The dose-response relationships of antipsychotic drugs for schizophrenia are not well defined, but such information would be important for decision making by clinicians." | ( Dose-Response Meta-Analysis of Antipsychotic Drugs for Acute Schizophrenia. Crippa, A; Davis, JM; Leucht, S; Orsini, N; Patel, MX; Siafis, S, 2020) | 0.56 |
" Dose-response curves were constructed with random-effects dose-response meta-analyses and a spline model." | ( Dose-Response Meta-Analysis of Antipsychotic Drugs for Acute Schizophrenia. Crippa, A; Davis, JM; Leucht, S; Orsini, N; Patel, MX; Siafis, S, 2020) | 0.56 |
" For some drugs, higher than currently licensed doses might be tested in further trials, because their dose-response curves did not plateau." | ( Dose-Response Meta-Analysis of Antipsychotic Drugs for Acute Schizophrenia. Crippa, A; Davis, JM; Leucht, S; Orsini, N; Patel, MX; Siafis, S, 2020) | 0.56 |
" Approved AL doses and dosing regimens include 441 mg monthly, 662 mg monthly, and 882 mg monthly or every 6 weeks (q6wk), as well as the most recently approved dose, 1064 mg, administered every 2 months." | ( Pharmacokinetics, Safety, and Tolerability of a 2-Month Dose Interval Regimen of the Long-Acting Injectable Antipsychotic Aripiprazole Lauroxil: Results From a 44-Week Phase I Study. Du, Y; Hard, M; Marandi, M; von Moltke, L; Walling, DP; Wehr, A; Weiden, PJ, 2020) | 0.77 |
"This study evaluated pharmacokinetics of AL given at a higher dosage strength (1064 mg) and at a longer dose interval (every 8 weeks [q8wk]) than previously studied." | ( Pharmacokinetics, Safety, and Tolerability of a 2-Month Dose Interval Regimen of the Long-Acting Injectable Antipsychotic Aripiprazole Lauroxil: Results From a 44-Week Phase I Study. Du, Y; Hard, M; Marandi, M; von Moltke, L; Walling, DP; Wehr, A; Weiden, PJ, 2020) | 0.77 |
"AL 1064 mg q8wk provided continuous exposure to aripiprazole throughout the 8-week dosing interval and had a safety profile consistent with the 4- and 6-week regimens." | ( Pharmacokinetics, Safety, and Tolerability of a 2-Month Dose Interval Regimen of the Long-Acting Injectable Antipsychotic Aripiprazole Lauroxil: Results From a 44-Week Phase I Study. Du, Y; Hard, M; Marandi, M; von Moltke, L; Walling, DP; Wehr, A; Weiden, PJ, 2020) | 0.77 |
" AL has five regimen options that offer three different injection intervals using four different dosage strengths." | ( Aripiprazole Lauroxil Dosing Regimens: Understanding Dosage Strengths and Injection Intervals. Du, Y; Faldu, S; Rege, B; Sommi, RW; Wehr, A; Weiden, PJ, 2022) | 2.16 |
Role | Description |
---|---|
H1-receptor antagonist | H1-receptor antagonists are the drugs that selectively bind to but do not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine. |
second generation antipsychotic | Antipsychotic drugs which can have different modes of action but which tend to be less likely than first generation antipsychotics to cause extrapyramidal motor control disabilities such as body rigidity or Parkinson's disease-type movements. |
serotonergic agonist | An agent that has an affinity for serotonin receptors and is able to mimic the effects of serotonin by stimulating the physiologic activity at the cell receptors. Serotonin agonists are used as antidepressants, anxiolytics, and in the treatment of migraine disorders. |
prodrug | A compound that, on administration, must undergo chemical conversion by metabolic processes before becoming the pharmacologically active drug for which it is a prodrug. |
[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] |
Class | Description |
---|---|
dodecanoate ester | Any fatty acid ester in which the carboxylic acid component is lauric acid. |
quinolone | |
dichlorobenzene | Any member of the class of chlorobenzenes carrying two chloro groups at unspecified positions. |
N-arylpiperazine | |
N-alkylpiperazine | |
aromatic ether | Any ether in which the oxygen is attached to at least one aryl substituent. |
delta-lactam | A lactam in which the amide bond is contained within a six-membered ring, which includes the amide nitrogen and the carbonyl carbon. |
[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] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 0 (0.00) | 29.6817 |
2010's | 24 (72.73) | 24.3611 |
2020's | 9 (27.27) | 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 (54.59) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 18 (50.00%) | 5.53% |
Reviews | 8 (22.22%) | 6.00% |
Case Studies | 0 (0.00%) | 4.05% |
Observational | 1 (2.78%) | 0.25% |
Other | 9 (25.00%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
---|---|---|---|---|---|---|---|
A Phase 3b, Multicenter, Randomized, Double-blind Study to Evaluate the Efficacy and Safety of Aripiprazole Lauroxil or Paliperidone Palmitate for the Treatment of Schizophrenia in Subjects Hospitalized for Acute Exacerbation [NCT03345979] | Phase 3 | 200 participants (Actual) | Interventional | 2017-11-15 | Completed | ||
Aripiprazole Lauroxil for Preventing Psychotic Relapse After an Initial Schizophrenia Episode [NCT04203056] | Phase 4 | 15 participants (Actual) | Interventional | 2019-12-16 | Terminated(stopped due to Withdraw of financial support by industry collaborator) | ||
A Phase 1, Randomized, Open-Label Study Evaluating the Pharmacokinetics of Various Dosing Regimens of Aripiprazole Lauroxil in Subjects With Stable Schizophrenia [NCT02320032] | Phase 1 | 140 participants (Actual) | Interventional | 2014-12-31 | Completed | ||
Safety and Tolerability of Initiating Aripiprazole Lauroxil in Subjects With Schizophrenia Who Are Inadequately Treated With Paliperidone Palmitate or Risperidone Long Acting Injection [NCT02634320] | Phase 4 | 51 participants (Actual) | Interventional | 2015-12-31 | Completed | ||
A Phase 1, Randomized, Open-label, Single Dose Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of Aripiprazole Lauroxil Following Administration to the Deltoid or Gluteal Muscle in Adults With Schizophrenia or Schizoaffective Disorder [NCT02636842] | Phase 1 | 47 participants (Actual) | Interventional | 2015-12-31 | Completed | ||
Comprehensive Treatment of Early Course Schizophrenia: A Nonrandomized Study of Long Acting Injectable Antipsychotic Medication Combined With Cognitive and Functional Skills Training [NCT05662306] | Phase 4 | 60 participants (Anticipated) | Interventional | 2024-02-01 | Recruiting | ||
[information is prepared from clinicaltrials.gov, extracted Sep-2024] |