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A Phase I Study of LXS196 in Patients With Metastatic Uveal Melanoma.

Phase 1
Terminated
Conditions
Uveal Melanoma
Interventions
Drug: LXS196 and HDM201
Registration Number
NCT02601378
Lead Sponsor
Novartis Pharmaceuticals
Brief Summary

This study was to characterize the safety, tolerability, pharmacokinetics (PK), pharmacodynamics (PD) and preliminary anti-tumor activity of LXS196 as a single agent and in combination with HDM201 in patients with metastatic uveal melanoma.

Detailed Description

Not available

Recruitment & Eligibility

Status
TERMINATED
Sex
All
Target Recruitment
107
Inclusion Criteria
  • Male or female patients ≥18 years of age
  • Diagnosis of uveal melanoma with histological or cytological confirmed metastatic disease. Disease must be treatment naive or have progressed (radiologically or clinically) on most recent therapy.
  • Willingness to provide newly obtained tumor tissue at baseline and on treatment unless contraindicated by medical risk in the opinion of the treating physician.
  • Measurable disease, defined as at least one lesion that can be accurately measured in at least one dimension (longest diameter to be recorded) as > 20 mm with conventional techniques or as >10 mm with CT scan.
  • ECOG performance status ≤ 1

Key

Exclusion Criteria
  • Malignant disease other than that being treated in this study.
  • Symptomatic or untreated CNS metastases or spinal cord compression. Brain metastasis must be stable with verification by imaging .
  • Impaired cardiac function or clinically significant cardiac diseases
  • History of thromboembolic or cerebrovascular events within the last 6 months, including transient ischemic attack, cerebrovascular accident, deep vein thrombosis, or pulmonary embolism (applicable to combination part only).
  • Patients who are receiving treatment with medications that cannot be discontinued prior to study entry and that are considered to be any of the following:
  • known and possible risk for QT prolongation
  • known to be strong inducers or inhibitors of CYP3A4/5 (for single agent part); known to be moderate to strong inducers or inhibitors of CYP3A4/5 (for combination part)
  • known to be inducers or inhibitors of P-gp
  • known to be substrates of CYP3A4/5 and P-gp with a narrow therapeutic index
  • Patients with abnormal laboratory values, defined as any of the following:
  • AST or ALT > 3 times ULN, AST or ALT > 5 times ULN for patients with liver metastases.
  • Total bilirubin > 1.5 x ULN, except for patients with Gilbert's syndrome who are excluded if total bilirubin > 3.0 x ULN or direct bilirubin > 1.5 x ULN.
  • Absolute neutrophil count (ANC) ≤ 1.5 x109/L.
  • Platelets ≤ 100 x 109/L.
  • Hemoglobin (Hgb) ≤ 90 g/L (9 g/dL).
  • Creatinine > 1.5 x ULN
  • Patients receiving live vaccines due to the expected bone marrow toxicity (applicable to combination part only).
  • Patients treated with growth factors targeting the myeloid lineage (e.g. G-CSF, GM-CSF and M-CSF) within 2 weeks of starting study treatment. (applicable to combination part only).

Study & Design

Study Type
INTERVENTIONAL
Study Design
SINGLE_GROUP
Arm && Interventions
GroupInterventionDescription
LXS196 as a single agentLXS196About 68 patients will be enrolled in dose escalation and expansion
LXS196 in combination with HDM201LXS196 and HDM201about 44 patients to be enrolled in dose escalation and expansion
Primary Outcome Measures
NameTimeMethod
Incidence of dose limiting toxicities (DLTs) (Dose escalation only)Cycle 1 in dose escalation

cycle = 28 days

Incidence and severity of adverse events and serious adverse events, including changes in laboratory parameters, vital signs and ECGs graded as per NCI CTCAE version 4.03 (All patients)Continuously throughout the study until 30 days after treatment discontinuation
Dose interruptions, reductions and dose intensityContinuously throughout the study until 30 days after treatment discontinuation
Secondary Outcome Measures
NameTimeMethod
Overall response rate (ORR) per RECIST version 1.1 criteriaFrom baseline, every 2 cycles until cycle 11, then every 3 cycles afterwards until disease progression or withdrawal of consent up to 12 months
Plasma LXS196 concentration-time profiles as a single agentCycle 1 Day 1, 2, 3, 15; Cycle 2, 3, 4, 5 and 6 Day1
Progression free survival (PFS) per RECIST version 1.1 criteriaFrom baseline, every 2 cycles until cycle 11, then every 3 cycles afterwards until disease progression or withdrawal of consent up to 12 months
Plasma PK parameters of LXS196 as a single agent:AUCCycle 1 Day 1, 2, 3, 15; Cycle 2, 3, 4, 5 and 6 Day1
Plasma PK parameters of LXS196 as a single agent: CmaxCycle 1 Day 1, 2, 3, 15; Cycle 2, 3, 4, 5 and 6 Day1
Plasma PK parameters of LXS196 as a single agent: TmaxCycle 1 Day 1, 2, 3, 15; Cycle 2, 3, 4, 5 and 6 Day1
Modulation of signaling molecules downstream of PKCBaseline and Cycle 1 Day 15
Plasma PK parameters of LXS196 as a single agent: t1/2Cycle 1 Day 1, 2, 3, 15; Cycle 2, 3, 4, 5 and 6 Day1
Plasma PK parameters of LXS196 as a single agent: RaccCycle 1 Day 1, 2, 3, 15; Cycle 2, 3, 4, 5 and 6 Day1
Plasma HDM201 concentration-time profilesCycle 1 Day 1, 2, 3, 8; Cycle 2, 3, 4, 5 and 6 Day 1
Plasma PK parameters of HDM201: AUCCycle 1 Day 1, 2, 3, 8; Cycle 2, 3, 4, 5 and 6 Day 1
Plasma PK parameters of HDM201: CmaxCycle 1 Day 1, 2, 3, 8; Cycle 2, 3, 4, 5 and 6 Day 1
Plasma PK parameters of HDM201: TmaxCycle 1 Day 1, 2, 3, 8; Cycle 2, 3, 4, 5 and 6 Day 1
Plasma PK parameters of HDM201: t1/2Cycle 1 Day 1, 2, 3, 8; Cycle 2, 3, 4, 5 and 6 Day 1
Plasma LXS196 concentration-time profiles in combination with HDM201Cycle 1 Day 1, 2, 3, 8; Cycle 2, 3, 4, 5 and 6 Day1
Plasma PK parameters of LXS196 in combination with HDM201:AUCCycle 1 Day 1, 2, 3, 8; Cycle 2, 3, 4, 5 and 6 Day1
Plasma PK parameters of LXS196 in combination with HDM201: CmaxCycle 1 Day 1, 2, 3, 8; Cycle 2, 3, 4, 5 and 6 Day1
Plasma PK parameters of LXS196 in combination with HDM201: TmaxCycle 1 Day 1, 2, 3, 8; Cycle 2, 3, 4, 5 and 6 Day1
Plasma PK parameters of LXS196 in combination with HDM201: t1/2Cycle 1 Day 1, 2, 3, 8; Cycle 2, 3, 4, 5 and 6 Day1
Plasma PK parameters of LXS196 in combination with HDM201: RaccCycle 1 Day 1, 2, 3, 8; Cycle 2, 3, 4, 5 and 6 Day1
LXS196 plasma protein binding as a single agentCycle 1 Day 1, 2, 15, 16
LXS196 plasma protein content as a single agentCycle 1, 2, 3 and 4 Day 1

Trial Locations

Locations (2)

Columbia University Medical Center

🇺🇸

New York, New York, United States

Novartis Investigative Site

🇪🇸

Madrid, Spain

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