Paclitaxel trevatide (formerly known as ANG 1005 or GRN 1005) is a paclitaxel-peptide drug conjugate, where three paclitaxel molecules linked by a cleavable succinyl ester linkage to a brain peptide vector, Angiopep-2. Paclitaxel trevatide is an oncology product to leverage the low-density lipoprotein receptor-related protein 1 (LRP-1) pathway to cross the blood-brain barrier (BBB) and enter cancer cells. This drug successfully completed phase II clinical trials in breast cancer patients with recurrent brain metastases and in patients with high-grade glioma. 30-May-2014 Angiochem, the company that developed this drug, announced that the Food & Drug Association (FDA) had granted both orphan drug and fast track designation to paclitaxel trevatide for the treatment of glioblastoma multiforme (GBM). In addition, paclitaxel trevatide is going to be involved in phase III clinical trial to see if this drug can prolong survival compared to a Physician Best Choice control in HER2-negative breast cancer patients with the newly diagnosed leptomeningeal disease and previously treated brain metastases.
CNS Activity
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| ANG1005 for breast cancer brain metastases: correlation between 18F-FLT-PET after first cycle and MRI in response assessment. | 2016-11 |
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| Phase I study of GRN1005 in recurrent malignant glioma. | 2013-03-15 |
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| Antitumour activity of ANG1005, a conjugate between paclitaxel and the new brain delivery vector Angiopep-2. | 2008-09 |
Sample Use Guides
In Vivo Use Guide
Sources: https://clinicaltrials.gov/ct2/show/NCT01967810
ANG1005 (PACLITAXEL TREVATIDE) at a starting dose of 650 mg/m2 by intravenous infusion once every 3 weeks
Route of Administration:
Intravenous
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ACTIVE MOIETY |
Structural Modifications
| Modification Type | Location Site | Location Type | Residue Modified | Extent | Fragment Name | Fragment Approval |
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| AMINO_ACID_SUBSTITUTION | [1_10] [1_15] | LYSINE | (N-SUCCINYL-PACLITAXEL)-LYSINE | HOY02N12D8 | ||
| AMINO_ACID_SUBSTITUTION | [1_1] | THREONINE | (N-SUCCINYL-PACLITAXEL)-THREONINE | G331NQ4LC1 |
| Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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| MOL_WEIGHT:NUMBER(CALCULATED) | CHEMICAL |
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| Molecular Formula | CHEMICAL |
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