Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C47H51NO14 |
Molecular Weight | 853.9061 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 11 / 11 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
[H][C@@]12C[C@H](O)[C@@]3(C)C(=O)[C@H](OC(C)=O)C4=C(C)[C@H](C[C@@](O)([C@@H](OC(=O)C5=CC=CC=C5)[C@]3([H])[C@@]1(CO2)OC(C)=O)C4(C)C)OC(=O)[C@H](O)[C@@H](NC(=O)C6=CC=CC=C6)C7=CC=CC=C7
InChI
InChIKey=RCINICONZNJXQF-MZXODVADSA-N
InChI=1S/C47H51NO14/c1-25-31(60-43(56)36(52)35(28-16-10-7-11-17-28)48-41(54)29-18-12-8-13-19-29)23-47(57)40(61-42(55)30-20-14-9-15-21-30)38-45(6,32(51)22-33-46(38,24-58-33)62-27(3)50)39(53)37(59-26(2)49)34(25)44(47,4)5/h7-21,31-33,35-38,40,51-52,57H,22-24H2,1-6H3,(H,48,54)/t31-,32-,33+,35-,36+,37+,38-,40-,45+,46-,47+/m0/s1
Molecular Formula | C47H51NO14 |
Molecular Weight | 853.9061 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 10 / 11 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
DescriptionSources: http://www.drugbank.ca/drugs/DB01229Curator's Comment: Description was created based on several sources, including http://www.accessdata.fda.gov/drugsatfda_docs/label/2011/020262s049lbl.pdf and https://www.ncbi.nlm.nih.gov/pubmed/18068131
Sources: http://www.drugbank.ca/drugs/DB01229
Curator's Comment: Description was created based on several sources, including http://www.accessdata.fda.gov/drugsatfda_docs/label/2011/020262s049lbl.pdf and https://www.ncbi.nlm.nih.gov/pubmed/18068131
Paclitaxel is a mitotic inhibitor used in cancer chemotherapy. It was discovered in a US National Cancer Institute program at the Research Triangle Institute in 1967 when Monroe E. Wall and Mansukh C. Wani isolated it from the bark of the Pacific yew tree, Taxus brevifolia and named it taxol. Later it was discovered that endophytic fungi in the bark synthesize paclitaxel. When it was developed commercially by Bristol-Myers Squibb (BMS), the generic name was changed to paclitaxel and the BMS compound is sold under the trademark Taxol. In this formulation, paclitaxel is dissolved in Kolliphor EL and ethanol, as a delivery agent. Taxol is marketed for the treatment of Breast cancer; Gastric cancer; Kaposi's sarcoma; Non-small cell lung cancer; Ovarian cancer. A newer formulation, in which paclitaxel is bound to albumin, is sold under the trademark Abraxane. 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. 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. 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.
CNS Activity
Sources: https://www.ncbi.nlm.nih.gov/pubmed/12056715
Curator's Comment: No or negligible penetration of paclitaxel over an intact blood– brain barrier
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: HeLa cell growth Sources: https://www.ncbi.nlm.nih.gov/pubmed/27095936 |
7.08 µM [IC50] | ||
Target ID: SKOV3 breast cancer cell growth Sources: https://www.ncbi.nlm.nih.gov/pubmed/27599579 |
38.7 nM [IC50] | ||
Target ID: GO:0046785 Sources: https://www.ncbi.nlm.nih.gov/pubmed/8555181 |
23.0 µM [EC50] | ||
Target ID: CHEMBL1915 Sources: http://www.drugbank.ca/drugs/DB01229 |
|||
Target ID: CHEMBL4860 Sources: http://www.drugbank.ca/drugs/DB01229 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | TAXOL Approved UseTAXOL is indicated as first-line and subsequent therapy for the treatment of advanced carcinoma of the ovary. Launch Date1998 |
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Primary | TAXOL Approved UseTAXOL is indicated for the treatment of breast cancer after failure of combination chemotherapy for metastatic disease or relapse within 6 months of adjuvant chemotherapy. Launch Date1998 |
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Primary | TAXOL Approved UseTAXOL, in combination with cisplatin, is indicated for the first-line treatment of nonsmall cell lung cancer in patients who are not candidates for potentially curative surgery and/or radiation therapy. Launch Date1998 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
6.92 μM EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/8664192 |
250 mg/m² steady-state, intravenous dose: 250 mg/m² route of administration: Intravenous experiment type: STEADY-STATE co-administered: |
PACLITAXEL plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
0.5 μM EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/7799018 |
175 mg/m² steady-state, intravenous dose: 175 mg/m² route of administration: Intravenous experiment type: STEADY-STATE co-administered: |
PACLITAXEL plasma | Homo sapiens population: UNKNOWN age: ADULT sex: FEMALE food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
27.07 μM × h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/8664192 |
250 mg/m² steady-state, intravenous dose: 250 mg/m² route of administration: Intravenous experiment type: STEADY-STATE co-administered: |
PACLITAXEL plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
14.8 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/7799018 |
175 mg/m² steady-state, intravenous dose: 175 mg/m² route of administration: Intravenous experiment type: STEADY-STATE co-administered: |
PACLITAXEL plasma | Homo sapiens population: UNKNOWN age: ADULT sex: FEMALE food status: UNKNOWN |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
6.5% |
PACLITAXEL plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
135 mg/m2 1 times / 3 weeks multiple, intravenous Recommended Dose: 135 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 135 mg/m2, 1 times / 3 weeks Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
Other AEs: Anaphylaxis, Dyspnea... Other AEs: Anaphylaxis (2%) Sources: Dyspnea (severe, 2%) Hypotension (severe, 2%) Generalized urticaria (severe, 2%) Angioedema (severe, 2%) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Anaphylaxis | 2% | 135 mg/m2 1 times / 3 weeks multiple, intravenous Recommended Dose: 135 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 135 mg/m2, 1 times / 3 weeks Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
Angioedema | severe, 2% | 135 mg/m2 1 times / 3 weeks multiple, intravenous Recommended Dose: 135 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 135 mg/m2, 1 times / 3 weeks Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
Dyspnea | severe, 2% | 135 mg/m2 1 times / 3 weeks multiple, intravenous Recommended Dose: 135 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 135 mg/m2, 1 times / 3 weeks Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
Generalized urticaria | severe, 2% | 135 mg/m2 1 times / 3 weeks multiple, intravenous Recommended Dose: 135 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 135 mg/m2, 1 times / 3 weeks Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
Hypotension | severe, 2% | 135 mg/m2 1 times / 3 weeks multiple, intravenous Recommended Dose: 135 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 135 mg/m2, 1 times / 3 weeks Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://www.jci.org/articles/view/15451 Page: - |
no |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2005/21660_ABRAXANE_biopharmr.PDF#page=20 Page: 20.0 |
major | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2005/21660_ABRAXANE_biopharmr.PDF#page=20 Page: 20.0 |
minor | |||
Page: - |
no | |||
Page: - |
yes [Km 6.79 uM] | |||
Page: - |
yes | |||
Sources: https://www.nature.com/articles/tpj201013 Page: - |
yes | |||
Sources: https://www.jci.org/articles/view/96160 Page: - |
yes | |||
Page: - |
yes |
PubMed
Title | Date | PubMed |
---|---|---|
[Atrial fibrillation in a patient with non-small-cell carcinoma of the lung in the course of paclitaxel therapy]. | 1998 Sep-Oct |
|
Activity of standard and investigational cytotoxic drugs in primary cultures of tumor cells from patients with kidney and urinary bladder carcinomas. | 1999 Dec |
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Microtubule dysfunction induced by paclitaxel initiates apoptosis through both c-Jun N-terminal kinase (JNK)-dependent and -independent pathways in ovarian cancer cells. | 1999 Mar 19 |
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Phase II of doxorubicin/taxol in metastatic breast cancer. Argentine Multicenter Taxol Group. | 1999 May |
|
Dissecting cellular processes using small molecules: identification of colchicine-like, taxol-like and other small molecules that perturb mitosis. | 2000 Apr |
|
Schedule dependency of paclitaxel-induced neuropathy in mice: a morphological study. | 2000 Aug |
|
Doxorubicin and paclitaxel in advanced breast carcinoma: importance of prior adjuvant anthracycline therapy. | 2000 Dec 1 |
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Paclitaxel, cisplatin, and gemcitabine combination chemotherapy within a multidisciplinary therapeutic approach in metastatic nonsmall cell lung carcinoma. | 2000 Dec 15 |
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Description of a short-term Taxol-induced nociceptive neuropathy in rats. | 2000 Dec 29 |
|
Slow polymerization of Mycobacterium tuberculosis FtsZ. | 2000 Jul |
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Polymeric micellar paclitaxel phosphorylates Bcl-2 and induces apoptotic regression of androgen-independent LNCaP prostate tumors. | 2000 Jul 1 |
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Mechanism of paclitaxel activity in Kaposi's sarcoma. | 2000 Jul 1 |
|
Susceptibility to drug-induced apoptosis correlates with differential modulation of Bad, Bcl-2 and Bcl-xL protein levels. | 2000 Jun |
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Second-line chemotherapy with paclitaxel, cisplatin and gemcitabine in pre-treated sensitive cisplatin-based patients with advanced non-small cell lung cancer. | 2000 May-Jun |
|
A paclitaxel-containing chemotherapy does not cause central nervous adverse effects: a prospective study in patients with ovarian cancer. | 2000 Sep-Oct |
|
Doxorubicin and paclitaxel in the treatment of advanced breast cancer: efficacy and cardiac considerations. | 2001 |
|
Drug approval summaries: arsenic trioxide, tamoxifen citrate, anastrazole, paclitaxel, bexarotene. | 2001 |
|
In vivo metabolism of epothilone B in tumor-bearing nude mice: identification of three new epothilone B metabolites by capillary high-pressure liquid chromatography/mass spectrometry/tandem mass spectrometry. | 2001 |
|
Management of recurrent juvenile granulosa cell tumor of the ovary. | 2001 Apr |
|
HPV16-E6 enhances mitoxantrone sensitivity in a human ovarian cancer line: an isolated instance or a trend? | 2001 Apr |
|
Cell cycle-related changes in regulatory volume decrease and volume-sensitive chloride conductance in mouse fibroblasts. | 2001 Apr |
|
Connexin 43 (cx43) enhances chemotherapy-induced apoptosis in human glioblastoma cells. | 2001 Apr 1 |
|
Taxol-induced cell cycle arrest and apoptosis: dose-response relationship in lung cancer cells of different wild-type p53 status and under isogenic condition. | 2001 Apr 26 |
|
Biweekly gemcitabine, doxorubicin, and paclitaxel as first-line treatment in metastatic breast cancer. Final results from a phase II trial. | 2001 Feb |
|
Gemcitabine plus cisplatin in breast cancer. | 2001 Feb |
|
Selective drug resistant human osteosarcoma cell lines. | 2001 Feb |
|
Changes in glycosylation during Drosophila development. The influence of ecdysone on hemomucin isoforms. | 2001 Feb |
|
Disruption of microtubular cytoskeleton induced by cryptogein, an elicitor of hypersensitive response in tobacco cells. | 2001 Feb |
|
Study of multi-drug resistant mechanisms in a taxol-resistant hepatocellular carcinoma QGY-TR 50 cell line. | 2001 Feb 9 |
|
Phase I study of paclitaxel (Taxol) plus vinorelbine (Navelbine) in patients with untreated stage IIIb and IV non-small cell lung cancer. | 2001 Feb-Mar |
|
Cisplatin and vinorelbine as second-line chemotherapy in patients with advanced non-small cell lung cancer (NSCLC) resistant to taxol plus gemcitabine. | 2001 Feb-Mar |
|
Neurotoxicity associated with a regimen of carboplatin (AUC 5-6) and paclitaxel (175 mg/m2 over 3 h) employed in the treatment of gynecologic malignancies. | 2001 Jan |
|
Opposite effects of microtubule-stabilizing and microtubule-destabilizing drugs on biogenesis of mitochondria in mammalian cells. | 2001 Jan |
|
Vascular expression of polycystin-2. | 2001 Jan |
|
CD11b/CD18 acts in concert with CD14 and Toll-like receptor (TLR) 4 to elicit full lipopolysaccharide and taxol-inducible gene expression. | 2001 Jan 1 |
|
Cutting edge: Gln22 of mouse MD-2 is essential for species-specific lipopolysaccharide mimetic action of taxol. | 2001 Jan 1 |
|
Pretreatment with paclitaxel enhances apo-2 ligand/tumor necrosis factor-related apoptosis-inducing ligand-induced apoptosis of prostate cancer cells by inducing death receptors 4 and 5 protein levels. | 2001 Jan 15 |
|
Taxane-antibody conjugates afford potent cytotoxicity, enhanced solubility, and tumor target selectivity. | 2001 Jan 15 |
|
Antitumor synergy of CV787, a prostate cancer-specific adenovirus, and paclitaxel and docetaxel. | 2001 Jan 15 |
|
Dispersion of cyclin B mRNA aggregation is coupled with translational activation of the mRNA during zebrafish oocyte maturation. | 2001 Jan 15 |
|
Stimulation of taxol production and excretion in Taxus spp cell cultures by rare earth chemical lanthanum. | 2001 Jan 23 |
|
Enhanced taxol production and release in Taxus chinensis cell suspension cultures with selected organic solvents and sucrose feeding. | 2001 Jan-Feb |
|
Dynamic events are differently mediated by microfilaments, microtubules, and mitogen-activated protein kinase during porcine oocyte maturation and fertilization in vitro. | 2001 Mar |
|
Paclitaxel sensitization of multidrug-resistant cells to chemotherapy is independent of the cell cycle. | 2001 Mar 1 |
|
Effects of emulsifiers on the controlled release of paclitaxel (Taxol) from nanospheres of biodegradable polymers. | 2001 Mar 12 |
|
Paclitaxel restores radiation-induced apoptosis in a bcl-2-expressing, radiation-resistant lymphoma cell line. | 2001 Mar 15 |
|
P-glycoprotein efflux pump expression and activity in Calu-3 cells. | 2001 May |
|
Regulation of BRCA1 and BRCA2 transcript in response to cisplatin, adriamycin, taxol and ionising radiation is correlated to p53 functional status in ovarian cancer cell lines. | 2001 May-Jun |
Patents
Sample Use Guides
For previously untreated patients with carcinoma of the ovary, one of the following recommended regimens may be given every 3 weeks.
a.TAXOL (PACLITAXEL) administered intravenously over 3 hours at a dose of 175 mg/m2 followed by cisplatin at a dose of 75 mg/m2; or
b.TAXOL (PACLITAXEL) administered intravenously over 24 hours at a dose of 135 mg/m2 followed by cisplatin at a dose of 75 mg/m2
2) In patients previously treated with chemotherapy for carcinoma of the ovary, the recommended regimen is TAXOL (PACLITAXEL) 135 mg/m2 or 175 mg/m2 administered intravenously over 3 hours every 3 weeks.
Route of Administration:
Intravenous
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/27420038
Paclitaxel inhibited tubulin polymerization in the presence of MAPs in vitro with an IC50 value of 38.19 ± 3.33 uM in living cancer cells (Hela cells and human osteosarcoma U2OS cells).
Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 15:18:43 GMT 2023
by
admin
on
Fri Dec 15 15:18:43 GMT 2023
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Record UNII |
P88XT4IS4D
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Record Status |
Validated (UNII)
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Record Version |
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Classification Tree | Code System | Code | ||
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FDA ORPHAN DRUG |
270208
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FDA ORPHAN DRUG |
50190
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NDF-RT |
N0000175085
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LIVERTOX |
NBK548093
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FDA ORPHAN DRUG |
394813
Created by
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NCI_THESAURUS |
C67437
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EU-Orphan Drug |
EU/3/06/422
Created by
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FDA ORPHAN DRUG |
454014
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WHO-VATC |
QL01CD01
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FDA ORPHAN DRUG |
594217
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FDA ORPHAN DRUG |
469915
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FDA ORPHAN DRUG |
103497
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FDA ORPHAN DRUG |
186404
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FDA ORPHAN DRUG |
482015
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NDF-RT |
N0000175592
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FDA ORPHAN DRUG |
278309
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WHO-ESSENTIAL MEDICINES LIST |
8.2
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FDA ORPHAN DRUG |
384912
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FDA ORPHAN DRUG |
104797
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FDA ORPHAN DRUG |
454114
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EMA ASSESSMENT REPORTS |
PAXENE (WITHDRAWN: OVARIAN NEOPLASMS)
Created by
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CFR |
21 CFR 516.1684
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FDA ORPHAN DRUG |
290709
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FDA ORPHAN DRUG |
252907
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NCI_THESAURUS |
C1490
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WHO-ATC |
L01CD01
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EMA ASSESSMENT REPORTS |
ABRAXANE (AUTHORIZED: PANCREATIC NEOPLASMS)
Created by
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FDA ORPHAN DRUG |
291009
Created by
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EMA ASSESSMENT REPORTS |
PAXENE (WITHDRAWN: CARCINOMA, NON-SMALL-CELL LUNG)
Created by
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FDA ORPHAN DRUG |
141701
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FDA ORPHAN DRUG |
280409
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33069-62-4
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PRIMARY | |||
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100000085474
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P88XT4IS4D
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EE-62
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45863
Created by
admin on Fri Dec 15 15:18:43 GMT 2023 , Edited by admin on Fri Dec 15 15:18:43 GMT 2023
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D017239
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6839
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admin on Fri Dec 15 15:18:43 GMT 2023 , Edited by admin on Fri Dec 15 15:18:43 GMT 2023
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125973
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admin on Fri Dec 15 15:18:43 GMT 2023 , Edited by admin on Fri Dec 15 15:18:43 GMT 2023
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CHEMBL428647
Created by
admin on Fri Dec 15 15:18:43 GMT 2023 , Edited by admin on Fri Dec 15 15:18:43 GMT 2023
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DTXSID9023413
Created by
admin on Fri Dec 15 15:18:43 GMT 2023 , Edited by admin on Fri Dec 15 15:18:43 GMT 2023
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DB01229
Created by
admin on Fri Dec 15 15:18:43 GMT 2023 , Edited by admin on Fri Dec 15 15:18:43 GMT 2023
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2770
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admin on Fri Dec 15 15:18:43 GMT 2023 , Edited by admin on Fri Dec 15 15:18:43 GMT 2023
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P88XT4IS4D
Created by
admin on Fri Dec 15 15:18:43 GMT 2023 , Edited by admin on Fri Dec 15 15:18:43 GMT 2023
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7052
Created by
admin on Fri Dec 15 15:18:43 GMT 2023 , Edited by admin on Fri Dec 15 15:18:43 GMT 2023
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PACLITAXEL
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admin on Fri Dec 15 15:18:43 GMT 2023 , Edited by admin on Fri Dec 15 15:18:43 GMT 2023
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1491332
Created by
admin on Fri Dec 15 15:18:43 GMT 2023 , Edited by admin on Fri Dec 15 15:18:43 GMT 2023
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56946
Created by
admin on Fri Dec 15 15:18:43 GMT 2023 , Edited by admin on Fri Dec 15 15:18:43 GMT 2023
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SUB09583MIG
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admin on Fri Dec 15 15:18:43 GMT 2023 , Edited by admin on Fri Dec 15 15:18:43 GMT 2023
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C1411
Created by
admin on Fri Dec 15 15:18:43 GMT 2023 , Edited by admin on Fri Dec 15 15:18:43 GMT 2023
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36314
Created by
admin on Fri Dec 15 15:18:43 GMT 2023 , Edited by admin on Fri Dec 15 15:18:43 GMT 2023
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m8351
Created by
admin on Fri Dec 15 15:18:43 GMT 2023 , Edited by admin on Fri Dec 15 15:18:43 GMT 2023
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Paclitaxel
Created by
admin on Fri Dec 15 15:18:43 GMT 2023 , Edited by admin on Fri Dec 15 15:18:43 GMT 2023
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C495179
Created by
admin on Fri Dec 15 15:18:43 GMT 2023 , Edited by admin on Fri Dec 15 15:18:43 GMT 2023
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2044
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486610
Created by
admin on Fri Dec 15 15:18:43 GMT 2023 , Edited by admin on Fri Dec 15 15:18:43 GMT 2023
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ALTERNATIVE |
Related Record | Type | Details | ||
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TRANSPORTER -> SUBSTRATE | |||
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TRANSPORTER -> SUBSTRATE | |||
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METABOLIC ENZYME -> SUBSTRATE | |||
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TRANSPORTER -> SUBSTRATE | |||
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TRANSPORTER -> INHIBITOR | |||
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METABOLIC ENZYME -> SUBSTRATE | |||
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TRANSPORTER -> SUBSTRATE | |||
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METABOLIC ENZYME -> INDUCER | |||
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TRANSPORTER -> INDUCER |
Paclitaxel activates pregnane X receptor (PXR)
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TRANSPORTER -> INHIBITOR |
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METABOLIC ENZYME -> INDUCER |
Paclitaxel activates pregnane X receptor (PXR)
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TRANSPORTER -> SUBSTRATE |
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BINDER->LIGAND |
BINDING
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TRANSPORTER -> INHIBITOR | |||
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TRANSPORTER -> SUBSTRATE |
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PRODRUG -> METABOLITE ACTIVE |
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PRODRUG -> METABOLITE ACTIVE | |||
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METABOLITE -> PARENT |
In vitro studies with human liver microsomes and tissue slices showed that paclitaxel was metabolized primarily to 6α-hydroxypaclitaxel by CYP2C8; and to two minor metabolites, 3'-p-hydroxypaclitaxel and 6α, 3'-p-dihydroxypaclitaxel, by CYP3A4.
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Related Record | Type | Details | ||
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IMPURITY -> PARENT |
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IMPURITY -> PARENT |
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IMPURITY -> PARENT |
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IMPURITY -> PARENT |
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IMPURITY -> PARENT |
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IMPURITY -> PARENT |
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IMPURITY -> PARENT |
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IMPURITY -> PARENT |
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IMPURITY -> PARENT |
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IMPURITY -> PARENT | |||
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IMPURITY -> PARENT |
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IMPURITY -> PARENT |
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IMPURITY -> PARENT |
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IMPURITY -> PARENT |
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IMPURITY -> PARENT |
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Related Record | Type | Details | ||
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ACTIVE MOIETY |
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Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Biological Half-life | PHARMACOKINETIC |
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