Investigational Drug Details
| Drug ID: | D361 |
| Drug Name: | Paclitaxel |
| Synonyms: | |
| Type: | small molecule |
| DrugBank ID: | DB01229 |
| DrugBank Description: | Paclitaxel is a chemotherapeutic agent marketed under the brand name Taxol among others. Used as a treatment for various cancers, paclitaxel is a mitotic inhibitor that was first isolated in 1971 from the bark of the Pacific yew tree which contains endophytic fungi that synthesize paclitaxel. It is available as an intravenous solution for injection and the newer formulation contains albumin-bound paclitaxel marketed under the brand name Abraxane. |
| PubChem ID: | 36314 |
| CasNo: | 33069-62-4 |
| Repositioning for NAFLD: | Yes |
| SMILES: | [H][C@]12[C@H](OC(=O)C3=CC=CC=C3)[C@]3(O)C[C@H](OC(=O)[C@H](O)[C@@H](NC(=O)C4=CC=CC=C4)C4=CC=CC=C4)C(C)=C([C@@H](OC(C)=O)C(=O)[C@]1(C)[C@@H](O)C[C@H]1OC[C@@]21OC(C)=O)C3(C)C |
| Structure: |
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| InChiKey: | RCINICONZNJXQF-MZXODVADSA-N |
| Molecular Weight: | 853.9061 |
| DrugBank Targets: | Tubulin beta-1 chain; Apoptosis regulator Bcl-2; Microtubule-associated protein 4; Microtubule-associated protein 2; Microtubule-associated protein tau; Nuclear receptor subfamily 1 group I member 2 |
| DrugBank MoA: | Paclitaxel interferes with the normal function of microtubule growth. Whereas drugs like colchicine cause the depolymerization of microtubules in vivo, paclitaxel arrests their function by having the opposite effect; it hyper-stabilizes their structure. This destroys the cell's ability to use its cytoskeleton in a flexible manner. Specifically, paclitaxel binds to the β subunit of tubulin. Tubulin is the "building block" of mictotubules, and the binding of paclitaxel locks these building blocks in place. The resulting microtubule/paclitaxel complex does not have the ability to disassemble. This adversely affects cell function because the shortening and lengthening of microtubules (termed dynamic instability) is necessary for their function as a transportation highway for the cell. Chromosomes, for example, rely upon this property of microtubules during mitosis. Further research has indicated that paclitaxel induces programmed cell death (apoptosis) in cancer cells by binding to an apoptosis stopping protein called Bcl-2 (B-cell leukemia 2) and thus arresting its function. |
| DrugBank Pharmacology: | Paclitaxel is a taxoid antineoplastic agent indicated as first-line and subsequent therapy for the treatment of advanced carcinoma of the ovary, and other various cancers including breast cancer. Paclitaxel is a novel antimicrotubule agent that promotes the assembly of microtubules from tubulin dimers and stabilizes microtubules by preventing depolymerization. This stability results in the inhibition of the normal dynamic reorganization of the microtubule network that is essential for vital interphase and mitotic cellular functions. In addition, paclitaxel induces abnormal arrays or "bundles" of microtubules throughout the cell cycle and multiple asters of microtubules during mitosis. |
| DrugBank Indication: | Used in the treatment of Kaposi's sarcoma and cancer of the lung, ovarian, and breast. Abraxane® is specfically indicated for the treatment of metastatic breast cancer and locally advanced or metastatic non-small cell lung cancer. |
| Targets: | |
| Therapeutic Category: | |
| Clinical Trial Progress: | |
| Latest Progress: |
| Trial ID | Source ID | Phases | Status | Study Results | Start Date | Last Update Posted | |
|---|---|---|---|---|---|---|---|
| L3372 | NCT00563225 | PHASE3 | COMPLETED | NO | 2002-10 | 2007-11-26 | Details |
| L4205 | NCT00671424 | PHASE1 | COMPLETED | NO | 2008-03 | 2012-03-19 | Details |
| L4277 | NCT04080596 | PHASE1 | COMPLETED | NO | 2017-10-13 | 2019-09-06 | Details |
| L5205 | NCT02467790 | PHASE1 | UNKNOWN | NO | 2015-02 | 2016-01-26 | Details |
| L5817 | NCT01752985 | PHASE2 | TERMINATED | YES | 2013-03-18 | 2019-07-30 | Details |
| L6892 | NCT00806897 | COMPLETED | NO | 2009-01 | 2016-11-23 | Details |
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