Lyophilized formulation solutions and lyophilized formulations, methods and uses
By using tert-butanol and water as solvents and adding excipients such as sucrose or mannitol, the solution formulation of TH-302 lyophilized preparation was optimized, solving the problems of low drug loading and adverse reactions, and achieving a lyophilized preparation with high drug loading and safety.
Patent Information
- Application Number
- CN202280046255.4
- Authority / Receiving Office
- CN · China
- Patent Type
- Patents(China)
- Current Assignee / Owner
- Priority Date
- 2021-08-27
- Filing Date
- 2022-08-26
- Publication Date
- 2026-03-03
- Estimated Expiration
- 2042-08-26
AI Technical Summary
The existing TH-302 lyophilized formulation has too low a drug loading, which makes it inconvenient and costly to use in clinical practice. In addition, the adverse reactions caused by excipients in the concentrated injection increase the risk of adverse reactions for patients.
Using tert-butanol and water as solvents, and adding appropriate excipients such as sucrose or mannitol, the solution formulation of the lyophilized preparation is optimized to improve the solubility and drug loading of TH-302, and to avoid the use of excipients that may cause adverse reactions.
The TH-302 lyophilized formulation with high drug loading capacity has been developed, reducing the number of lyophilized formulations used in clinical practice, lowering the cost of medication for patients, and reducing the risk of adverse reactions.
Smart Images

Figure CN117651548B_ABST
Abstract
Citation Information
Patent Citations
Phosphoramidate alkylator prodrugs
CN101501054A
Compositions and methods for treating cancer
WO2004087075A2
Phosphoramidate alkylator prodrugs
WO2007002931A2
Phosphoramidate alkylator prodrugs for the treatment of cancer
WO2008083101A1
Hypoxia activated prodrugs of antineoplastic agents
WO2008151253A1