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NCT03520842

Regorafenib and Methotrexate in Treating Participants With Recurrent or Metastatic KRAS Mutated Non-Small Cell Lung Cancer

Completed Phase 2 Results posted Last updated 1 August 2023
What this trial tests

Phase 2 trial testing Methotrexate in KRAS Gene Mutation in 22 participants. Completed in 15 June 2022.

Timeline
14 August 2018
Primary endpoint
15 June 2022
15 June 2022

Quick facts

Lead sponsorStanford University
PhasePhase 2
StatusCompleted
Study typeINTERVENTIONAL
Allocationna
Designsingle group
Maskingnone
Primary purposetreatment
Enrollment22
Start date14 August 2018
Primary completion15 June 2022
Estimated completion15 June 2022
Sites1 location across United States

Drugs / interventions tested

Conditions studied

Sponsor

Stanford University

Who can join

18 and older, any sex, with KRAS Gene Mutation or Metastatic Malignant Neoplasm in the Brain. Patients with the condition only — healthy volunteers not accepted.

Results — posted to ClinicalTrials.gov

Per-arm endpoint measurements with 95% confidence intervals where reported. Source: trial results section.

Progression Free Survival (PFS) Primary · From first study treatment assessed up to 15 months

Progression free survival (PFS), measured from time of first study treatment until objective tumor progression as assessed by Response Evaluation Criteria in Solid Tumors (RECIST) version 1.1 criteria or death from any cause, whichever occurs earlier. PFS was calculated using the Kaplan-Meier method along with 95% confidence interval. RECIST v1.1 criteria are: * Complete Response (CR) = Disappearance of all target lesions * Partial Response (PR) = ≥ 30% decrease in the sum of the longest diameter of target lesions * Overall Response (OR) = CR + PR * Progressive disease (PD) = 20% increase in

GroupValue95% CI
Treatment (Regorafenib, Methotrexate)3.71.8 – 8.6
Objective Response Rate (ORR) Secondary · Up to 24 months

Objective response rate (ORR; as determined by RECIST v1.1) will be assessed as the proportion (percent) of participants with either complete response (CR; disappearance of all target lesions) or partial response (PR; ≥ 30% decrease in the sum of the longest diameter of target lesions), with exact 95% confidence intervals based on a binomial distribution.

GroupValue95% CI
Treatment (Regorafenib, Methotrexate)16.73.5 – 41.4
Disease Control Rate (DCR) Secondary · At 8 weeks

Disease control rate (DCR) will be assessed as the proportion of complete responses (CR) + partial responses (PR) + stable disease (SD) after 8 weeks of treatment (+/- 1 week), as determined by using RECIST v1.1

GroupValue95% CI
Treatment (Regorafenib, Methotrexate)66.741.0 – 86.7
Number of Participants With Adverse Events Secondary · Up to 38 months

Participants who experienced any treatment emergent adverse event and any ≥ grade 3 adverse event is reported.

Any grade
GroupValue95% CI
Treatment (Regorafenib, Methotrexate)17
≥ grade 3
GroupValue95% CI
Treatment (Regorafenib, Methotrexate)14
Trough Serum Concentration of Methotrexate Secondary · Cycle 1, Days 1, 8, 15, and 22

Pharmacokinetics (PK) of methotrexate when co-administered with regorafenib, as indicated by the trough serum concentration, was accessed by a fluorescent polarization immunoassay, and is reported as the mean with standard deviation. Participants treated with at least 1 dose of regorafenib and methotrexate and with at least one evaluable baseline pharmacokinetic sample and one follow up trough pharmacokinetic sample treated were included.

Cycle 1, Day 1
GroupValue95% CI
Treatment (Regorafenib, Methotrexate)0.04± 0.02
Cycle 1, Day 8
GroupValue95% CI
Treatment (Regorafenib, Methotrexate)0.04± 0.01
Cycle 1, Day 15
GroupValue95% CI
Treatment (Regorafenib, Methotrexate)0.05± 0.03
Cycle 1, Day 22
GroupValue95% CI
Treatment (Regorafenib, Methotrexate)0.05± 0.02
Maximum Serum Concentration (Cmax) of Methotrexate Secondary · Cycle 1, Days 1, 8, and 15

Pharmacokinetics (PK) of methotrexate when co-administered with regorafenib, as indicated by the maximum serum concentration (Cmax) of methotrexate, was assessed by a fluorescent polarization immunoassay, and is reported as the mean with standard deviation. Participants treated with at least 1 dose of regorafenib and methotrexate and with at least one evaluable Cmax pharmacokinetic sample were included in the assessment.

Cycle 1, Day 1
GroupValue95% CI
Treatment (Regorafenib, Methotrexate)0.43± 0.23
Cycle 1, Day 8
GroupValue95% CI
Treatment (Regorafenib, Methotrexate)0.60± 0.30
Cycle 1, Day 15
GroupValue95% CI
Treatment (Regorafenib, Methotrexate)0.60± 0.43

Adverse events — posted to ClinicalTrials.gov

Time frame: Up to 38 months. Reporting threshold: 0%. Adverse-event reports describe events observed during the trial — not all are caused by the drug.

Treatment (Regorafenib, Methotrexate)
Serious: 8/18 (44%)
Deaths: 2/18

Serious adverse events (10 terms)

ReactionSystemTreatment (Regorafenib, Me…
DyspneaRespiratory, thoracic and mediastinal disorders
HypoxiaRespiratory, thoracic and mediastinal disorders
AspirationRespiratory, thoracic and mediastinal disorders
PneumothoraxRespiratory, thoracic and mediastinal disorders
HemoptysisRespiratory, thoracic and mediastinal disorders
Abdominal painGastrointestinal disorders
Thromboembolic event: pulmonary embolismVascular disorders
Atrial fibrillationCardiac disorders
PancreatitisGastrointestinal disorders
Productive CoughRespiratory, thoracic and mediastinal disorders
Other adverse events (123 terms — click to expand)

ReactionSystemTreatment (Regorafenib, Me…
DyspneaRespiratory, thoracic and mediastinal disorders
FatigueGeneral disorders
HypophosphatemiaMetabolism and nutrition disorders
Mucositis oralGastrointestinal disorders
AnorexiaMetabolism and nutrition disorders
NauseaGastrointestinal disorders
Palmar-plantar erthryodysesthesia syndromeSkin and subcutaneous tissue disorders
HoarsenessRespiratory, thoracic and mediastinal disorders
PainGeneral disorders
DiarrheaGastrointestinal disorders
HypertensionVascular disorders
HyponatremiaMetabolism and nutrition disorders
MyalgiaMusculoskeletal and connective tissue disorders
PruritusSkin and subcutaneous tissue disorders
VomitingGastrointestinal disorders
Weight lossInvestigations
AlopeciaSkin and subcutaneous tissue disorders
ConstipationGastrointestinal disorders
Alanine aminotransferase increasedInvestigations
Amylase increasedInvestigations
Aspartate aminotransferase increasedInvestigations
Back painMusculoskeletal and connective tissue disorders
CoughRespiratory, thoracic and mediastinal disorders
DizzinessNervous system disorders
DysgeusiaNervous system disorders
DysphagiaGastrointestinal disorders
EpistaxisRespiratory, thoracic and mediastinal disorders
HeadacheNervous system disorders
HypokalemiaMetabolism and nutrition disorders
Lipase increasedInvestigations
Localized edemaGeneral disorders
Non-cardiac chest painMusculoskeletal and connective tissue disorders
Productive coughRespiratory, thoracic and mediastinal disorders
Blood bilirubin increasedInvestigations
Dry skinSkin and subcutaneous tissue disorders
Gastroesphogeal reflux diseaseGastrointestinal disorders
HypocalcemiaMetabolism and nutrition disorders
HypotensionVascular disorders
HypoxiaRespiratory, thoracic and mediastinal disorders
ParesthesiaNervous system disorders

Most-reported serious reactions: Dyspnea, Hypoxia, Aspiration, Pneumothorax, Hemoptysis, Abdominal pain, Thromboembolic event: pulmonary embolism, Atrial fibrillation.

Data from ClinicalTrials.gov NCT03520842 adverse events section.

Sponsor's own description

This phase II trial studies how well regorafenib works together with methotrexate in treating participants with metastatic non-squamous non-small cell lung cancer with tumors that harbor a KRAS mutation. Regorafenib is a targeted therapy that works on different cancer pathways to stop the growth of tumor cells and stop them from spreading. Methotrexate may stop the growth of tumor cells by blocking some of the enzymes needed for cell growth. Giving regorafenib and methotrexate together may work in treating participants with KRAS mutated non-small cell lung cancer.

Publications & conference data

8 peer-reviewed publications reference this trial (live from Europe PMC):

  1. Lipid Metabolism Regulates Oxidative Stress and Ferroptosis in RAS-Driven Cancers: A Perspective on Cancer Progression and Therapy.
    Bartolacci C, Andreani C, El-Gammal Y, Scaglioni PP. · · 2021 · cited 58× · PMID 34485382 · DOI 10.3389/fmolb.2021.706650
  2. KRAS Mutations in Solid Tumors: Characteristics, Current Therapeutic Strategy, and Potential Treatment Exploration.
    Yang Y, Zhang H, Huang S, Chu Q. · · 2023 · cited 50× · PMID 36675641 · DOI 10.3390/jcm12020709
  3. KRAS-Mutant Non-Small Cell Lung Cancer: An Emerging Promisingly Treatable Subgroup.
    Xie M, Xu X, Fan Y. · · 2021 · cited 46× · PMID 34012925 · DOI 10.3389/fonc.2021.672612
  4. Targeting KRAS in Solid Tumors: Current Challenges and Future Opportunities of Novel KRAS Inhibitors.
    Indini A, Rijavec E, Ghidini M, Cortellini A, et al · · 2021 · cited 37× · PMID 34064352 · DOI 10.3390/pharmaceutics13050653
  5. NSCLC as the Paradigm of Precision Medicine at Its Finest: The Rise of New Druggable Molecular Targets for Advanced Disease.
    Michelotti A, de Scordilli M, Bertoli E, De Carlo E, et al · · 2022 · cited 24× · PMID 35743191 · DOI 10.3390/ijms23126748
  6. Molecular Biology and Therapeutic Perspectives for K-Ras Mutant Non-Small Cell Lung Cancers.
    Cekani E, Epistolio S, Dazio G, Cefalì M, et al · · 2022 · cited 20× · PMID 36077640 · DOI 10.3390/cancers14174103
  7. Targeting KRAS in NSCLC: Old Failures and New Options for "Non-G12c" Patients.
    Jacobs F, Cani M, Malapelle U, Novello S, et al · · 2021 · cited 14× · PMID 34944952 · DOI 10.3390/cancers13246332
  8. Targeted therapies in non-small cell lung cancer: present and future.
    McLaughlin J, Berkman J, Nana-Sinkam P. · · 2023 · cited 11× · PMID 37675274 · DOI 10.12703/r/12-22

Verify or expand the search:

Other trials of Methotrexate

Trials testing the same drug.

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Currently open trials in the same condition.

Other Stanford University trials

Trials by the same sponsor.

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