[CAS NO. 1132936-00-5] ABT-072
PRODUCTS SPECIFICATIONS [1132936-00-5]
DESCRIPTION [1132936-00-5]
Overview
| MDL | MFCD28502074 |
|---|---|
| Molecular Weight | 469.55 |
| Molecular Formula | C24H27N3O5S |
| SMILES | CS(=O)(NC1=CC=C(/C=C/C2=CC(N(C(N3)=O)C=CC3=O)=CC(C(C)(C)C)=C2OC)C=C1)=O |
Summary
IC50 & Target
NS5B polymerase [1]
In Vitro
ABT-072 is a non-nucleoside NS5B polymerase inhibitor with nanomolar potency in vitro against genotype 1a and 1b hepatitis C virus polymerases [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
ABT-072 (5 and/or 30 mg/kg; i.v. or p.o.) shows good PK properties
[3]
.
ABT-072 (2.5 and/or 30 mg/kg; i.v. or p.o.) shows low plasma clearance and high oral bioavailability
[3]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Rats [3] |
| Dosage: | 5 and/or 30 mg/kg (Pharmacokinetic Analysis) |
| Administration: | I.v. or p.o. |
| Result: | Showed good PK properties. |
| Animal Model: | Dog [3] |
| Dosage: | 2.5 or 30 mg/kg (Pharmacokinetic Analysis) |
| Administration: | I.v. or p.o. |
| Result: | Showed low plasma clearance and high oral bioavailability. |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT00752687 | Abbott |
Hepatitis C
|
September 2008 | Phase 1 |
| NCT01221298 | AbbVie (prior sponsor, Abbott)|AbbVie |
Hepatitis C|HCV|Chronic Hepatitis C Infection|Hepatitis C Genotype 1
|
October 2010 | Phase 2 |
| NCT00947440 | Abbott |
Hepatitis C
|
July 2009 | Phase 1 |
| NCT00890318 | Abbott |
HCV Infection
|
April 2009 | Phase 1 |
| NCT00872196 | AbbVie (prior sponsor, Abbott)|AbbVie |
Hepatitis C Virus Infection
|
April 2009 | Phase 2 |
| NCT01074008 | AbbVie (prior sponsor, Abbott)|AbbVie |
Hepatitis C|HCV|Chronic Hepatitis C Infection|Hepatitis C Genotype 1
|
March 2010 | Phase 2 |
| NCT01081483 | Abbott|Abbott Japan Co.,Ltd |
Hepatitis C
|
March 2010 | Phase 1 |
| NCT00982826 | Abbott |
Hepatitis C
|
September 2009 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 80 mg/mL ( 170.38 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.1297 mL | 10.6485 mL | 21.2970 mL |
| 5 mM | 0.4259 mL | 2.1297 mL | 4.2594 mL |
| 10 mM | 0.2130 mL | 1.0648 mL | 2.1297 mL |
References
- [1] Lawitz E, et al. A phase 2a trial of 12-week interferon-free therapy with two direct-acting antivirals (ABT-450/r, ABT-072) and ribavirin in IL28B C/C patients with chronic hepatitis C genotype 1. J Hepatol. 2013;59(1):18-23.
- [2] Shi Y, et al. Assessing Supersaturation and Its Impact on In Vivo Bioavailability of a Low-Solubility Compound ABT-072 With a Dual pH, Two-Phase Dissolution Method. J Pharm Sci. 2016;105(9):2886-2895.
- [3] Randolph JT, et al. Synthesis and Biological Characterization of Aryl Uracil Inhibitors of Hepatitis C Virus NS5B Polymerase: Discovery of ABT-072, a trans-Stilbene Analog with Good Oral Bioavailability. J Med Chem. 2018;61(3):1153-1163.
