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TLD-1, a Novel Liposomal Doxorubicin, in Patients With Advanced Solid Tumors

Phase 1
Terminated
Conditions
Advanced Solid Tumors
Interventions
Registration Number
NCT03387917
Lead Sponsor
Swiss Group for Clinical Cancer Research
Brief Summary

TLD-1 is a novel liposomal formulation of doxorubicin (PEG surface) that compared favorably to conventional liposomal formulations of doxorubicin including Caelyx® in preclinical in vivo models. Particle features including size, charge distribution, lipid composition and drug release add up to a considerably altered particle behavior compared to Caelyx®, potentially explaining the lack of hand-foot-syndrome in respective animal models. Preclinical evaluation confirmed TLD-1 to be a promising new and innovative formulation of doxorubicin with promising activity and good tolerability.

Detailed Description

Despite impressive progress in the fields of surgical and immunological cancer therapies, most late-stage cancer treatments still heavily depend on conventional chemotherapeutics, which are often effective but also toxic, resulting in severe adverse effects limiting the dose and duration of therapy. Consequently, there remains a high unmet medical need for new innovative systemic treatments with an improved risk-benefit-profile.

Doxorubicin is a potent anthracycline used as a systemic treatment against several solid tumor including breast, ovarian and bladder cancer, small cell lung cancer and various types of sarcoma. However, Doxorubicin use is often limited due to hematological and non-hematological toxicity including cumulative cardiotoxicity with myocardial damage.

Cardiotoxicity has been substantially mitigated through the introduction of liposomal formulations such as Myocet and Caelyx/Doxil. Both products are associated with substantially lower rates of cardiac dysfunction during or post-treatment. Whereas Myocet's clinical use remains limited due to the intricate "bedside" reconstitution process, Caelyx has been associated with a high incidence of Palmar-Plantar Erythrodysesthesia (PPE) (also called hand-foot-syndrome), likely due to its long plasma half-life.

The development of TLD-1 (Talidox) aimed at combining the cardio-preserving properties of the liposomal delivery system with shorter blood circulation time in order to reduce the risk of PPE. Even though the pathophysiology of PPE is not yet fully understood, studies analyzing the correlation of dose and pharmacokinetic parameters with PLD toxic effects revealed that the severity of PPE correlated significantly with plasma half-life (t1/2).

Given its performance in preclinical trials, TLD-1 bears the potential for an improved benefit/risk profile compared to established liposomal doxorubicin formulations including Caelyx.

This first-in-human phase-I trial will evaluate the safety and will establish the maximal tolerated dose (MTD) and recommended phase II dose of TLD-1, and characterize specific dose limiting toxicities (DLT) of TLD-1. Moreover, the trial shall yield information on adverse events profile, pharmacokinetics and preliminary efficacy.

Recruitment & Eligibility

Status
TERMINATED
Sex
All
Target Recruitment
12
Inclusion Criteria

Not provided

Exclusion Criteria

Not provided

Study & Design

Study Type
INTERVENTIONAL
Study Design
SINGLE_GROUP
Arm && Interventions
GroupInterventionDescription
TLD-1TLD-1Duration of treatment * 1 cycle: 21 days * 1 cycle: 28 days (only comparative PK part, in cycle 1 or 2) * until progression or occurrence of unacceptable toxicity or withdrawal, but * maximum 9 cycles for patients previously not treated with anthracyclines * maximum 6 cycles for patients previously treated with anthracyclines. * Dose: i.v., according to DL on day 1 of each cycle or tentative MTD
Caelyx (only for comparative PK part)CaelyxDuration of treatment * 1 cycle: 28 days * Caelyx is given only in one cycle (cycle 1 or 2) * Dose: i.v., 40mg/m2
Primary Outcome Measures
NameTimeMethod
Dose-limiting toxicity (DLT)at 3 weeks
Descriptive pharmacokinetics (PK) of TLD-1 vs Caelyx: Area under curve [Cmax]2 months
Descriptive pharmacokinetics (PK) of TLD-1 vs Caelyx: Terminal half life [t½]2 months
Descriptive pharmacokinetics (PK) of TLD-1 vs Caelyx: Ratio of unencapsulated to encapsulated drug over time for Caelyx and TLD-12 months
Descriptive pharmacokinetics (PK) of TLD-1 vs Caelyx: volume of distribution [Vd]2 months
Descriptive pharmacokinetics (PK) of TLD-1 vs Caelyx: Area under curve [AUC]2 months
Descriptive pharmacokinetics (PK) of TLD-1 vs Caelyx: Clearance (CL)2 months
Secondary Outcome Measures
NameTimeMethod
Population pharmacokinetics: Area Under the Curve [AUC]at 2 months
Time to treatment failure (TTF)at 7 months
Adverse Events (AEs)at 7 months
Population pharmacokinetics (PK) of TLD-1: clearance (CL)at 2 months
Population pharmacokinetics: Maximum Plasma Concentration [Cmax]at 2 months
Objective tumor response (OR)at 7 months
Population pharmacokinetics (PK) of TLD-1: volume of distribution (Vd)at 2 months

Trial Locations

Locations (5)

Istituto Oncologico della Svizzera Italiana

🇨🇭

Bellinzona, Switzerland

Inselspital Bern

🇨🇭

Bern, Switzerland

Kantonsspital Graubünden

🇨🇭

Chur, Switzerland

Kantonsspital St. Gallen

🇨🇭

St. Gallen, Switzerland

Kantonsspital Winterthur

🇨🇭

Winterthur, Switzerland

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