larotaxel: has antineoplastic activity [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 6918260 |
| CHEMBL ID | 4279455 |
| SCHEMBL ID | 125697 |
| MeSH ID | M0524397 |
| Synonym |
|---|
| xrp-9881 |
| larotaxel |
| xrp9881 |
| pnu 100940 |
| benzenepropanoic acid, beta-(((1,1-dimethylethoxy)carbonyl)amino)-alpha-hydroxy-, (1s,2s,4s,7r,8ar,9as,10ar,12as,12br)-7,12a-bis(acetyloxy)-1-(benzoyloxy)-1,3,4,7,8,9,9a,10,10a,12,12a,12b-dodecahydro-2-hydroxy-5,13,13-trimethyl-8-oxo-2,6-methano-2h-cyclod |
| twq8k8a81y , |
| 156294-36-9 |
| unii-twq8k8a81y |
| xrp 9881 |
| larotaxel [inn] |
| 192573-38-9 |
| 1-hydroxy-9-oxo-5.beta.,20-epoxy-7.beta.,19-cyclotax-11-ene-2.alpha.,4,10.beta.,13.alpha.-tetrayl 4,10-diacetate 2-benzoate 13-((2r,3s)-3-((tert-butoxycarbonyl)amino)-2-hydroxy-3-phenylpropanoate) |
| larotaxel [who-dd] |
| SCHEMBL125697 |
| DXOJIXGRFSHVKA-BZVZGCBYSA-N |
| [(1s,2s,3r,4s,7r,9s,11r,13r,16s)-4,13-diacetyloxy-1-hydroxy-16-[(2r,3s)-2-hydroxy-3-[(2-methylpropan-2-yl)oxycarbonylamino]-3-phenylpropanoyl]oxy-15,18,18-trimethyl-12-oxo-6-oxapentacyclo[12.3.1.03,11.04,7.09,11]octadec-14-en-2-yl] benzoate |
| DB12984 |
| Q6489757 |
| (1s,2s,4s,7r,8ar,9as,10ar,12as,12br)-1-(benzoyloxy)-4-(((2r,3s)-3-((tert-butoxycarbonyl)amino)-2-hydroxy-3-phenylpropanoyl)oxy)-2-hydroxy-5,13,13-trimethyl-8-oxo-1,3,4,7,8,9,9a,10,10a,12b-decahydro-2h-2,6-methanocyclodeca[3,4]cyclopropa[4,5]benzo[1,2-b]ox |
| CS-0091011 |
| HY-125374 |
| larotaxel (dihydrate) |
| xrp9881 (dihydrate) |
| benzenepropanoic acid, beta-[[(1,1-dimethylethoxy)carbonyl]amino]-alpha-hydroxy-, (1s,2s,4s,7r,8ar,9as,10ar,12as,12br)-7,12a-bis(acetyloxy)-1-(benzoyloxy)-1,3,4,7,8,9,9a,10,10a,12,12a,12b-dodecahydro-2-hydroxy-5,13,13-trimethyl-8-oxo-2,6-methano-2h-cyclod |
| CHEMBL4279455 |
| AKOS040741938 |
Larotaxel is a new chemical structure drug, which has not been marketed worldwide. It is a taxane analog that has the potential for the treatment of various types of cancer.
The validated method was successfully applied to a pharmacokinetic study of larotaxel in beagle dogs after intravenous administration of larOTaxel-loaded lipid microsphere with different doses of 0.1 mg/ml. The method was also successfully applied for the pharmacokinetics study of Larotaxal in rat plasma after a single intravenous injection.
| Excerpt | Reference | Relevance |
|---|---|---|
| " The validated method was successfully applied to the pharmacokinetic study of larotaxel in rat plasma after a single intravenous administration of larotaxel injection and larotaxel-loaded liposome, respectively." | ( Cloud-point extraction combined with HPLC for determination of larotaxel in rat plasma: a pharmacokinetic study of liposome formulation. Liu, Y; Ma, H; You, J, 2012) | 0.85 |
| " The quantitation method was successfully applied for simultaneous estimation of LTX and its metabolites in a pharmacokinetic study after oral administration at different doses of 10, 20, and 40 mg/kg and intravenous administration at the dose 10 mg/kg to Wistar rats, respectively." | ( Determination of larotaxel and its metabolites in rat plasma by liquid chromatography-tandem mass spectrometry: application for a pharmacokinetic study. Bi, K; Chen, X; Hou, P; Ju, P; Liu, Z; Tang, X; Zhang, L; Zhang, Y, 2014) | 0.74 |
A new taxane, larotaxel (XRP9881), was tested in lung cancer patients. It was found to be effective in combination with either cisplatin or gemcitabine. The combination had the most promising antitumor activity.
| Excerpt | Reference | Relevance |
|---|---|---|
| "This randomized phase II study investigated the efficacy and safety of a new taxane, larotaxel (XRP9881), in combination with either cisplatin or gemcitabine in the first-line treatment of patients with nonirradiable stage IIIB or stage IV non-small cell lung cancer to select the combination having the most promising antitumor activity." | ( Randomized multicenter phase II study of larotaxel (XRP9881) in combination with cisplatin or gemcitabine as first-line chemotherapy in nonirradiable stage IIIB or stage IV non-small cell lung cancer. Besenval, M; Bosquee, L; Brain, E; Dansin, E; Dohollou, N; Gervais, R; Quoix, E; Sessa, C; Urban, T; Vansteenkiste, J; Zatloukal, P, 2008) | 0.84 |
| "Both larotaxel combinations were effective and manageable, however all measured efficacy parameters (response rate, progression free survival, and survival) seemed to favor the combination with cisplatin." | ( Randomized multicenter phase II study of larotaxel (XRP9881) in combination with cisplatin or gemcitabine as first-line chemotherapy in nonirradiable stage IIIB or stage IV non-small cell lung cancer. Besenval, M; Bosquee, L; Brain, E; Dansin, E; Dohollou, N; Gervais, R; Quoix, E; Sessa, C; Urban, T; Vansteenkiste, J; Zatloukal, P, 2008) | 1.13 |
| "This primary objective of this phase I dose-escalation study was to define the maximum tolerated dose (MTD) and dose limiting toxicity (DLT) of larotaxel administered in combination with carboplatin in chemotherapy-naïve patients with advanced/metastatic non-small cell lung cancer (NSCLC)." | ( A phase I study of larotaxel (XRP9881) administered in combination with carboplatin in chemotherapy-naïve patients with stage IIIB or stage IV non-small cell lung cancer. Ackerman, J; Gupta, S; Harper, K; Robert, F, 2010) | 0.89 |
| "A simple and efficient method based on cloud-point extraction combined with high-performance liquid chromatography was developed and validated for the determination of larotaxel in rat plasma." | ( Cloud-point extraction combined with HPLC for determination of larotaxel in rat plasma: a pharmacokinetic study of liposome formulation. Liu, Y; Ma, H; You, J, 2012) | 0.81 |
Larotaxel has linear pharmacokinetic characteristics in rats after oral administration. The absolute bioavailability of LTX delivered by solid lipid loaded nanoparticles was found to be 13.
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1406313 | Cell cycle arrest in human A549 cells assessed as accumulation at S phase at 40 nM after 24 hrs by RNase A/propidium iodide staining-based flow cytometric analysis (Rvb = 13.4%) | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Synthesis and biological evaluation of novel larotaxel analogues. |
| AID1406312 | Cell cycle arrest in human A549 cells assessed as accumulation at G1 phase at 40 nM after 24 hrs by RNase A/propidium iodide staining-based flow cytometric analysis (Rvb = 58.0%) | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Synthesis and biological evaluation of novel larotaxel analogues. |
| AID1406309 | Cytotoxicity against human A549 cells after 72 hrs by sulforhodamine B assay | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Synthesis and biological evaluation of novel larotaxel analogues. |
| AID1406306 | Cytotoxicity against human MCF7 cells after 72 hrs by sulforhodamine B assay | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Synthesis and biological evaluation of novel larotaxel analogues. |
| AID1406308 | Resistance factor, ratio of IC50 for human MCF7/ADR cells to IC50 for human MCF7 cells | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Synthesis and biological evaluation of novel larotaxel analogues. |
| AID1406305 | Resistance factor, ratio of IC50 for human KB/VCR cells to IC50 for human KB cells | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Synthesis and biological evaluation of novel larotaxel analogues. |
| AID1406311 | Resistance factor, ratio of IC50 for human paclitaxl resistant A549 cells to IC50 for human A549 cells | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Synthesis and biological evaluation of novel larotaxel analogues. |
| AID1406310 | Cytotoxicity against human paclitaxl resistant A549 cells after 72 hrs by sulforhodamine B assay | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Synthesis and biological evaluation of novel larotaxel analogues. |
| AID1406307 | Cytotoxicity against human MCF7/ADR cells after 72 hrs by sulforhodamine B assay | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Synthesis and biological evaluation of novel larotaxel analogues. |
| AID1406314 | Cell cycle arrest in human A549 cells assessed as accumulation at G2/M phase at 40 nM after 24 hrs by RNase A/propidium iodide staining-based flow cytometric analysis (Rvb = 58.0%) | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Synthesis and biological evaluation of novel larotaxel analogues. |
| AID1406303 | Cytotoxicity against human KB/VCR cells after 72 hrs by sulforhodamine B assay | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Synthesis and biological evaluation of novel larotaxel analogues. |
| AID1406304 | Cytotoxicity against human KB cells after 72 hrs by sulforhodamine B assay | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Synthesis and biological evaluation of novel larotaxel analogues. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 3 (13.64) | 29.6817 |
| 2010's | 16 (72.73) | 24.3611 |
| 2020's | 3 (13.64) | 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 (22.22) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 4 (18.18%) | 5.53% |
| Reviews | 3 (13.64%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 15 (68.18%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||