Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C19H22O7S |
| Molecular Weight | 394.439 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 1 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
COC1=CC(OC)=C(\C=C\S(=O)(=O)CC2=CC(O)=C(OC)C=C2)C(OC)=C1
InChI
InChIKey=GHPUSRLWNSTQIK-BQYQJAHWSA-N
InChI=1S/C19H22O7S/c1-23-14-10-18(25-3)15(19(11-14)26-4)7-8-27(21,22)12-13-5-6-17(24-2)16(20)9-13/h5-11,20H,12H2,1-4H3/b8-7+
Briciclib (also known as ON-013105 and ON-014185) has the potential of targeting and inhibition of eukaryotic translation initiation factor 4E (eIF4E) for solid cancers. eIF4E is a proto-oncogene that promotes translation of several genes essential for cellular proliferation (cyclin D1, c-Myc, mTOR), survival (Akt), angiogenesis (VEGF), and metastasis (MMP9). Overexpression of eIF4E has been observed in almost all major groups of cancers and has been shown to induce increased expression of cyclin D1 and c-Myc). An intravenous formulation of briciclib was being investigated in the Phase 1 clinical trial. The purpose of the study was to determine the highest dose of briciclib that could be given safely in patients with relapsed/refractory Lymphoma or B-cell Acute Lymphocytic Leukemia (Philadelphia chromosome negative). However, this study was terminated because of the lack of available clinical drug supply. In addition, briciclib was also involved in phase I clinical trials with advanced cancer and solid tumors, to determine the highest dose that can be safely given.
Originator
Approval Year
Sample Use Guides
The starting dose of briciclib in the Escalation Stage will be 17 mg/week, with subsequent dose escalation levels of 35 mg, 70 mg, 140 mg, 280 mg, 560 mg, and 1120 mg. At each dose level, briciclib will be administered as a 2-hour intravenous infusion, once-a-week per 3-week cycles.
Route of Administration:
Intravenous
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J3I19I491A
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11269418
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865783-95-5
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952304-24-4
Created by
admin on Mon Mar 31 21:29:00 GMT 2025 , Edited by admin on Mon Mar 31 21:29:00 GMT 2025
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NON-SPECIFIC STEREOCHEMISTRY |
ACTIVE MOIETY
PRODRUG (METABOLITE ACTIVE)
