Teverelix-TFA Dosage Regime for Prostate Cancer
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Solution Overview
Problem
Current dosage regimes for teverelix-TFA in treating prostate cancer are less effective in maintaining castration levels over a long treatment period, leading to side effects such as cardiovascular diseases.
Innovation Solution
A dosage regime comprising a loading dose of 360 mg subcutaneously and 180 mg intramuscularly, administered simultaneously, followed by maintenance doses of 360 mg subcutaneously every six weeks, to achieve and maintain castration levels in prostate cancer patients.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Object-affected harmful factors
If relatively low doses of teverelix are used to reduce side effects, then adverse events are reduced, but the therapeutic effect is insufficient and patients do not remain castrated throughout the treatment period
Solution Approach 1:
The treatment is divided into two distinct phases: an initial loading phase with higher doses (360-480 mg) to achieve rapid castration and suppress adverse events, followed by a maintenance phase with lower doses (120-180 mg) to sustain castration levels. This segmentation allows optimization of both safety and efficacy at different treatment stages.
Solution Approach 2:
A loading dose is administered before the maintenance phase to pre-establish therapeutic drug levels in the body. This preliminary high-dose administration ensures rapid achievement of castration levels, preventing the flare effect and reducing adverse events before the lower maintenance doses begin.
2Reliability
If multiple individual injections are administered on several consecutive days to achieve therapeutic effect, then castration levels are achieved, but patient compliance decreases and treatment complexity increases
Solution Approach 1:
Multiple dose administrations that would traditionally be given on separate consecutive days are merged into a single combined injection event. The loading phase may involve two injections given within a short window (same day or consecutive days), and maintenance phases are administered as single injections every 4-8 weeks, significantly reducing the burden on patients.
Solution Approach 2:
The extended-release formulation ensures continuous therapeutic drug levels are maintained in the body over the treatment period. The drug is released gradually from the injection site, providing sustained castration effect without requiring frequent re-administration, thus maintaining continuous therapeutic action with minimal patient intervention.
3Reliability
If GnRH agonists are used for androgen deprivation therapy, then treatment is effective, but cardiovascular diseases and other adverse events occur at higher rates
Solution Approach 1:
The patent changes the fundamental pharmacological parameter from GnRH agonist stimulation to GnRH antagonist blockade. Teverelix directly blocks GnRH receptors, preventing the flare effect and achieving rapid, sustained suppression of luteinizing hormone and testosterone without the cardiovascular adverse events associated with agonist therapy. This parameter change maintains treatment effectiveness while improving safety profile.
Data Source
Figure 1A~1B
Figure 2~3
AI summary
The present invention relates to a dosage regime for a teverelix-TFA composition used for treating prostate cancer. Said dosage regime comprises a loading dose of 360 mg SC and 180 mg IM, with a low maintenance dose of the teverelix-TFA composition (360 mg SC) every six weeks starting at day 28. Thus, the dosage regime according to the invention provides an improve dosage regimens in which a castration rate of ≥95% is obtained in a treatment period of 52 weeks, and with fewer side effects and adverse events, thereby providing an optimised response/side effect relationship.