| MDL | - |
|---|---|
| Molecular Weight | 438.60 |
| Molecular Formula | C27H38N2O3 |
| SMILES | O=C(NN(C(C1=CC(C)=CC(C)=C1)=O)[C@@H](C(C)(C)C)CCC)C2=CC=CC(OC)=C2CC |
Veledimex (INXN-1001), a synthetic analog of the insect molting hormone ecdysone, is an orally active activator ligand for a proprietary gene therapy promoter system. Veledimex can be used to activate certain genes using the ecdysone receptor (EcR)-based inducible gene regulation system, the RheoSwitch Therapeutic System (RTS). Veledimex can cross blood-brain barrier (BBB) in both orthotopic GL-261 mice and cynomolgus monkeys [1] [2] .
|
IL-12 |
Veledimex (INXN-1001) generally has moderate to low oral bioavailability after a single oral administration in mice and monkeys (-56% in mice and up to 17.4% in cynomolgus monkeys) with mostly low plasma clearance (1399 and 1170 mL/h per kilogram in mice and monkeys, respectively), high volume of distribution (20271 and 9180 mL/h per kilogram in mice and monkeys, respectively), and long terminal half-lives (-10 hours in mice and -30 hours in monkeys) after intravenous administration [1] . Ad-RTS-mIL-12 + Veledimex have demonstrated a dose-related increase in tumor IL-12 mRNA and IL-12 protein expression. Discontinuation of Veledimex resulted in a return to baseline IL-12 mRNA and protein expression in numerous syngeneic mouse tumor models. Veledimex crosses the blood-brain-barrier in both naive and orthotopic GL-261 mice with increased brain tissue level of -6 fold observed in tumor bearing vs. normal mice. Ad-RTS-mIL-12 + veledimex demonstrate a dose-related increase in survival without significant adverse events [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT02423902 | Alaunos Therapeutics |
Metastatic Breast Cancer
|
July 2015 | Phase 1|Phase 2 |
| NCT04006119 | Alaunos Therapeutics |
Glioblastoma
|
August 1, 2019 | Phase 2 |
| NCT01397708 | Alaunos Therapeutics |
Melanoma
|
August 2011 | Phase 1|Phase 2 |
| NCT02026271 | Alaunos Therapeutics |
Glioblastoma Multiforme|Anaplastic Oligoastrocytoma
|
June 2015 | Phase 1 |
| NCT00815607 | Alaunos Therapeutics |
Melanoma
|
April 2009 | Phase 1 |
| NCT03679754 | Alaunos Therapeutics |
Glioblastoma
|
September 5, 2018 | Phase 1 |
| NCT03636477 | Alaunos Therapeutics |
Glioblastoma
|
June 18, 2018 | Phase 1 |
| NCT01703754 | Alaunos Therapeutics |
Breast Cancer Nos Metastatic Recurrent
|
March 2013 | Phase 2 |
| NCT03740724 | Castle Creek Biosciences, LLC. |
Morphea|Scleroderma, Localized|Scleroderma
|
December 18, 2019 | Phase 1|Phase 2 |
| NCT03330197 | Alaunos Therapeutics |
Pediatric Brain Tumor|Diffuse Intrinsic Pontine Glioma
|
September 26, 2017 | Phase 1|Phase 2 |
Solid
Room temperature in continental US; may vary elsewhere.
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
DMSO : 25 mg/mL ( 57.00 mM ; Need ultrasonic)
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.2800 mL | 11.3999 mL | 22.7998 mL |
| 5 mM | 0.4560 mL | 2.2800 mL | 4.5600 mL |
| 10 mM | 0.2280 mL | 1.1400 mL | 2.2800 mL |
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.70 mM); Clear solution