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NCT01295827: KEYNOTE-001

Study of Pembrolizumab (MK-3475) in Participants With Progressive Locally Advanced or Metastatic Carcinoma, Melanoma, or Non-small Cell Lung Carcinoma (P07990/MK-3475-001/KEYNOTE-001)

Completed Phase 1 Results posted Last updated 13 December 2019
What this trial tests

Phase 1 trial testing Pembrolizumab in Cancer, Solid Tumor in 1,260 participants. Completed in 11 December 2018.

Timeline
4 March 2011
Primary endpoint
5 November 2018
11 December 2018

Quick facts

Lead sponsorMerck Sharp & Dohme LLC
PhasePhase 1
StatusCompleted
Study typeINTERVENTIONAL
Allocationrandomized
Designparallel
Maskingnone
Primary purposetreatment
Enrollment1,260
Start date4 March 2011
Primary completion5 November 2018
Estimated completion11 December 2018

Drugs / interventions tested

Conditions studied

Sponsor

Merck Sharp & Dohme LLC — full company profile →

Who can join

18 and older, any sex, with Cancer, Solid Tumor. 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.

Number of Participants Experiencing Dose-Limiting Toxicities (DLTs) According to National Cancer Institute Common Terminology Criteria for Adverse Events Version 4.0 (NCI-CTCAE v.4.0) in Participants With Solid Tumors (Parts A and A1) Primary · Up to 28 days in Cycle 1

DLTs were assessed according to NCI-CTCAE v.4.0 during the first cycle (28 days) and were defined as occurrence of any of the following toxicities if judged by the investigator to be possibly, probably or definitely related to study drug administration: Grade (Gr) 4 nonhematologic toxicity; Gr 4 hematologic toxicity lasting ≥14 days; Gr 3 nonhematologic toxicity lasting \>3 days despite optimal supportive care; any Grade 3 non-hematologic laboratory value if medical intervention was required to treat the participant, the abnormality led to hospitalization, or the abnormality persisted for \>1

GroupValue95% CI
Solid Tumors: Pembrolizumab 1 mg/kg Q2W (Part A)0
Solid Tumors: Pembrolizumab 3 mg/kg Q2W (Part A)0
Solid Tumors: Pembrolizumab 10 mg/kg Q2W (Parts A+A1)0
Number of Participants Who Experienced an Adverse Event (AE) Primary · Up to approximately 91 months (through Final Database cut-off date of 05-Nov-2018)

An AE was defined as any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of the Sponsor's product, whether or not considered related to the use of the product. Any worsening (i.e., any clinically significant adverse change in frequency and/or intensity) of a pre-existing condition which was temporally associated with the use of the Sponsor's product was also an AE. The number of participants who experienced an AE was reported for each arm.

GroupValue95% CI
Solid Tumors: Pembrolizumab 1 mg/kg Q2W (Part A)4
Solid Tumors: Pembrolizumab 3 mg/kg Q2W (Part A)3
Solid Tumors: Pembrolizumab 10 mg/kg Q2W (Parts A+A1)9
Solid Tumors: Pembrolizumab Titration Cohort 1 Q3W (Part A2)4
Solid Tumors: Pembrolizumab Titration Cohort 2 Q3W (Part A2)3
Solid Tumors: Pembrolizumab Titration Cohort 3 Q3W (Part A2)6
MEL: Pembrolizumab 2 mg/kg Q3W (Parts B+D)161
MEL: Pembrolizumab 10 mg/kg Q3W (Parts B+D)308
MEL: Pembrolizumab 10 mg/kg Q2W (Part B)178
NSCLC: Pembrolizumab 2 mg/kg Q3W (Part F)60
NSCLC: Pembrolizumab 10 mg/kg Q3W (Parts C+F)277
NSCLC: Pembrolizumab 10 mg/kg Q2W (Part F)198
Overall Response Rate (ORR) According to Response Evaluation Criteria In Solid Tumors Version 1.1 (RECIST 1.1) as Assessed by Integrated Radiology and Oncology (IRO): Melanoma Participants (Parts B Plus D) Primary · Up to approximately 53 months (through Interim Database cut-off date of 18-Sep-2015)

ORR was defined as the percentage of participants in the analysis population who had a confirmed Complete Response (CR: disappearance of all lesions) or Partial Response (PR: at least a 30% decrease in the sum of diameters \[SOD\] of target lesions, taking as reference the baseline SOD) according to RECIST 1.1, which was modified for this study to follow a maximum of 10 target lesions and a maximum of 5 target lesions per organ. The percentage of participants who experienced a confirmed CR or PR according to RECIST 1.1 as assessed by IRO was reported as the ORR for each melanoma dose arm (Part

GroupValue95% CI
MEL: Pembrolizumab 2 mg/kg Q3W (Parts B+D)30.223.3 – 37.9
MEL: Pembrolizumab 10 mg/kg Q3W (Parts B+D)29.424.4 – 34.8
MEL: Pembrolizumab 10 mg/kg Q2W (Part B)36.729.6 – 44.2
ORR According to RECIST 1.1 as Assessed by Independent Review Committee (IRC): Non-Small Cell Lung Cancer (NSCLC) Participants (Parts C Plus F) Primary · Up to approximately 53 months (through Interim Database cut-off date of 18-Sep-2015)

ORR was defined as the percentage of participants in the analysis population who had a confirmed CR (disappearance of all lesions) or PR (at least a 30% decrease in the sum of diameters \[SOD\] of target lesions, taking as reference the baseline SOD) according to RECIST 1.1, which was modified for this study to follow a maximum of 10 target lesions and a maximum of 5 target lesions per organ. The percentage of participants who experienced a confirmed CR or PR according to RECIST 1.1 as assessed by IRC was reported as the ORR for each NSCLC dose arm (Parts C plus F).

GroupValue95% CI
NSCLC: Pembrolizumab 2 mg/kg Q3W (Part F)19.710.6 – 31.8
NSCLC: Pembrolizumab 10 mg/kg Q3W (Parts C+F)21.617.0 – 26.8
NSCLC: Pembrolizumab 10 mg/kg Q2W (Part F)19.314.1 – 25.4
ORR According to Immune-related Response Criteria (irRC) as Assessed by Investigator in Melanoma Participants (Parts B Plus D) Secondary · Up to approximately 53 months (through Interim Database cut-off date of 18-Sep-2015)

ORR was defined as the percentage of participants in the analysis population who had a confirmed immune-related Complete Response (irCR: complete disappearance of all tumor lesions whether measurable or not, and no new lesions) or immune-related Partial Response (irPR: decrease in sum of the products of the two largest perpendicular diameters (SPD) of ≥50% by a consecutive assessment ≥4 weeks after first documentation) according to irRC. The percentage of participants who experienced a confirmed irCR or irPR according to irRC as assessed by the investigator was reported as the ORR for each mel

GroupValue95% CI
MEL: Pembrolizumab 2 mg/kg Q3W (Parts B+D)35.227.9 – 43.1
MEL: Pembrolizumab 10 mg/kg Q3W (Parts B+D)39.934.5 – 45.6
MEL: Pembrolizumab 10 mg/kg Q2W (Part B)45.638.1 – 53.1
ORR According to irRC as Assessed by Investigator in NSCLC Participants (Parts C Plus F) Secondary · Up to approximately 53 months (through Interim Database cut-off date of 18-Sep-2015)

ORR was defined as the percentage of participants in the analysis population who had a confirmed irCR (complete disappearance of all tumor lesions whether measurable or not, and no new lesions) or irPR (decrease in sum of the products of the two largest perpendicular diameters (SPD) of ≥50% by a consecutive assessment ≥4 weeks after first documentation) according to irRC. The percentage of participants who experienced a confirmed irCR or irPR according to irRC as assessed by the investigator was reported as the ORR for each NSCLC dose arm (Parts C plus F).

GroupValue95% CI
NSCLC: Pembrolizumab 2 mg/kg Q3W (Part F)23.013.2 – 35.5
NSCLC: Pembrolizumab 10 mg/kg Q3W (Parts C+F)28.923.7 – 34.5
NSCLC: Pembrolizumab 10 mg/kg Q2W (Part F)22.316.7 – 28.6
Area Under the Concentration-Time Curve of Pembrolizumab From Time 0 to Day 28 (AUC 0-28) in Solid Tumor Participants (Parts A and A1) Secondary · Cycle 1: Pre-dose, post-dose at 0.5, 6, 24, and 48 hours and Days 8, 15, and 22 (Cycle 1 = 28 days)

Blood samples were collected at specified intervals for the determination of AUC0-28. AUC0-28 was defined as the area under the concentration-time curve of pembrolizumab from time zero to Day 28. AUC0-28 was based on noncompartmental analysis and reported for participants in Parts A and A1.

GroupValue95% CI
Solid Tumors: Pembrolizumab 1 mg/kg Q2W (Part A)157± 16
Solid Tumors: Pembrolizumab 3 mg/kg Q2W (Part A)955± 23
Solid Tumors: Pembrolizumab 10 mg/kg Q2W (Parts A+A1)2160± 31
Area Under the Concentration-Time Curve of Pembrolizumab From Time 0 to Infinity (AUC 0-inf) in Solid Tumor Participants (Parts A and A1) Secondary · Cycle 1: Pre-dose, post-dose at 0.5, 6, 24, and 48 hours and Days 8, 15, and 22 (Cycle 1 = 28 days)

Blood samples were collected at specified intervals for the determination of AUC0-inf. AUC0-inf was defined as the area under the concentration-time curve of pembrolizumab from time zero to infinity. AUC0-inf was based on noncompartmental analysis and reported for participants in Parts A and A1.

GroupValue95% CI
Solid Tumors: Pembrolizumab 1 mg/kg Q2W (Part A)212± 36
Solid Tumors: Pembrolizumab 3 mg/kg Q2W (Part A)1530± 28
Solid Tumors: Pembrolizumab 10 mg/kg Q2W (Parts A+A1)3230± 44
Maximum Concentration (Cmax) of Pembrolizumab in Solid Tumor Participants (Parts A and A1) Secondary · Cycle 1: Pre-dose, post-dose at 0.5, 6, 24, and 48 hours and Days 8, 15, and 22 (Cycle 1 = 28 days)

Blood samples were collected at specified intervals for the determination of Cmax. Cmax was defined as the maximum concentration of pembrolizumab reached. Cmax was based on noncompartmental analysis and reported for participants in Parts A and A1.

GroupValue95% CI
Solid Tumors: Pembrolizumab 1 mg/kg Q2W (Part A)16.4± 22
Solid Tumors: Pembrolizumab 3 mg/kg Q2W (Part A)107± 26
Solid Tumors: Pembrolizumab 10 mg/kg Q2W (Parts A+A1)256± 37
Time to Maximum Concentration (Tmax) of Pembrolizumab in Solid Tumor Participants (Parts A and A1) Secondary · Cycle 1: Pre-dose, post-dose at 0.5, 6, 24, and 48 hours and Days 8, 15, and 22 (Cycle 1 = 28 days)

Blood samples were collected at specified intervals for the determination of Tmax. Tmax was defined as time to the maximum concentration of pembrolizumab reached. Tmax was based on noncompartmental analysis and reported for participants in Parts A and A1.

GroupValue95% CI
Solid Tumors: Pembrolizumab 1 mg/kg Q2W (Part A)0.050.02 – 0.17
Solid Tumors: Pembrolizumab 3 mg/kg Q2W (Part A)0.170.17 – 0.17
Solid Tumors: Pembrolizumab 10 mg/kg Q2W (Parts A+A1)0.170.03 – 0.99
Terminal Half-Life (t ½) of Pembrolizumab in Solid Tumor Participants (Parts A and A1) Secondary · Cycle 1: Pre-dose, post-dose at 0.5, 6, 24, and 48 hours and Days 8, 15, and 22 (Cycle 1 = 28 days)

Blood samples were collected at specified intervals for the determination of t½. t½ was defined as the time required to divide the pembrolizumab plasma concentration by two after reaching pseudo-equilibrium, following a single dose of pembrolizumab. t½ was based on noncompartmental analysis and reported for participants in Parts A and A1.

GroupValue95% CI
Solid Tumors: Pembrolizumab 1 mg/kg Q2W (Part A)14.1± 51
Solid Tumors: Pembrolizumab 3 mg/kg Q2W (Part A)21.6± 10
Solid Tumors: Pembrolizumab 10 mg/kg Q2W (Parts A+A1)17.5± 54
Area Under the Concentration-Time Curve of Pembrolizumab From Time 0 to Day 21 (AUC 0-21) in Solid Tumor Participants (Part A2) Secondary · Cycle 1: Day 1: Pre-dose, post-dose at 0.5, 6, 24, and 48 hours; Day 5, Day 8: pre- and post-dose; Day 15 (Cycle = 21 days)

Blood samples were collected at specified intervals for the determination of AUC0-21. AUC0-21 was defined as the area under the concentration-time curve of pembrolizumab from time zero to Study Day 21. AUC0-21 was based on noncompartmental analysis and reported for participants in Part A2.

GroupValue95% CI
Solid Tumors: Pembrolizumab Titration Cohort 1 Q3W (Part A2)57.1± 21
Solid Tumors: Pembrolizumab Titration Cohort 2 Q3W (Part A2)50.4± 28
Solid Tumors: Pembrolizumab Titration Cohort 3 Q3W (Part A2)186± 28

Adverse events — posted to ClinicalTrials.gov

Time frame: Up to approximately 91 months (through Final Database cut-off date of 05-Nov-2018). Reporting threshold: 5%. Adverse-event reports describe events observed during the trial — not all are caused by the drug.

Solid Tumors: Pembrolizumab 1 mg/kg Q2W (Part A)
Serious: 1/4 (25%)
Deaths: 2/4
Solid Tumors: Pembrolizumab 3 mg/kg Q2W (Part A)
Serious: 1/3 (33%)
Deaths: 1/3
Solid Tumors: Pembrolizumab 10 mg/kg Q2W (Parts A+A1)
Serious: 3/10 (30%)
Deaths: 6/12
Solid Tumors: Pembrolizumab Titration Cohort 1 Q3W (Part A2)
Serious: 0/4 (0%)
Deaths: 2/4
Solid Tumors: Pembrolizumab Titration Cohort 2 Q3W (Part A2)
Serious: 2/3 (67%)
Deaths: 1/3
Solid Tumors: Pembrolizumab Titration Cohort 3 Q3W (Part A2)
Serious: 2/6 (33%)
Deaths: 5/6
MEL: Pembrolizumab 2 mg/kg Q3W (Parts B+D)
Serious: 69/162 (43%)
Deaths: 111/164
MEL: Pembrolizumab 10 mg/kg Q3W (Parts B+D)
Serious: 129/313 (41%)
Deaths: 213/321
MEL: Pembrolizumab 10 mg/kg Q2W (Part B)
Serious: 79/180 (44%)
Deaths: 110/183
NSCLC: Pembrolizumab 2 mg/kg Q3W (Part F)
Serious: 34/61 (56%)
Deaths: 52/61
NSCLC: Pembrolizumab 10 mg/kg Q3W (Parts C+F)
Serious: 119/287 (41%)
Deaths: 240/296
NSCLC: Pembrolizumab 10 mg/kg Q2W (Part F)
Serious: 86/202 (43%)
Deaths: 166/203

Serious adverse events (343 terms)

ReactionSystemSolid Tumors: Pembrolizuma…Solid Tumors: Pembrolizuma…Solid Tumors: Pembrolizuma…Solid Tumors: Pembrolizuma…Solid Tumors: Pembrolizuma…Solid Tumors: Pembrolizuma…MEL: Pembrolizumab 2 mg/kg…MEL: Pembrolizumab 10 mg/k…MEL: Pembrolizumab 10 mg/k…NSCLC: Pembrolizumab 2 mg/…NSCLC: Pembrolizumab 10 mg…NSCLC: Pembrolizumab 10 mg…
Pleural effusionRespiratory, thoracic and mediastinal disorders
PneumoniaInfections and infestations
Squamous cell carcinomaNeoplasms benign, malignant and unspecified (incl cysts and polyps)
DyspnoeaRespiratory, thoracic and mediastinal disorders
CellulitisInfections and infestations
Basal cell carcinomaNeoplasms benign, malignant and unspecified (incl cysts and polyps)
Pulmonary embolismRespiratory, thoracic and mediastinal disorders
PneumonitisRespiratory, thoracic and mediastinal disorders
Atrial fibrillationCardiac disorders
ColitisGastrointestinal disorders
NauseaGastrointestinal disorders
PyrexiaGeneral disorders
Chronic obstructive pulmonary diseaseRespiratory, thoracic and mediastinal disorders
Respiratory failureRespiratory, thoracic and mediastinal disorders
Abdominal painGastrointestinal disorders
DiarrhoeaGastrointestinal disorders
Gastrointestinal haemorrhageGastrointestinal disorders
Urinary tract infectionInfections and infestations
HaemoptysisRespiratory, thoracic and mediastinal disorders
PneumothoraxRespiratory, thoracic and mediastinal disorders
AnaemiaBlood and lymphatic system disorders
Lung infectionInfections and infestations
SepsisInfections and infestations
HyponatraemiaMetabolism and nutrition disorders
Acute kidney injuryRenal and urinary disorders
Other adverse events (128 terms — click to expand)

ReactionSystemSolid Tumors: Pembrolizuma…Solid Tumors: Pembrolizuma…Solid Tumors: Pembrolizuma…Solid Tumors: Pembrolizuma…Solid Tumors: Pembrolizuma…Solid Tumors: Pembrolizuma…MEL: Pembrolizumab 2 mg/kg…MEL: Pembrolizumab 10 mg/k…MEL: Pembrolizumab 10 mg/k…NSCLC: Pembrolizumab 2 mg/…NSCLC: Pembrolizumab 10 mg…NSCLC: Pembrolizumab 10 mg…
FatigueGeneral disorders
DiarrhoeaGastrointestinal disorders
NauseaGastrointestinal disorders
PruritusSkin and subcutaneous tissue disorders
ArthralgiaMusculoskeletal and connective tissue disorders
CoughRespiratory, thoracic and mediastinal disorders
Decreased appetiteMetabolism and nutrition disorders
RashSkin and subcutaneous tissue disorders
DyspnoeaRespiratory, thoracic and mediastinal disorders
HeadacheNervous system disorders
ConstipationGastrointestinal disorders
VomitingGastrointestinal disorders
AnaemiaBlood and lymphatic system disorders
Oedema peripheralGeneral disorders
Back painMusculoskeletal and connective tissue disorders
AstheniaGeneral disorders
PyrexiaGeneral disorders
MyalgiaMusculoskeletal and connective tissue disorders
VitiligoSkin and subcutaneous tissue disorders
ChillsGeneral disorders
Pain in extremityMusculoskeletal and connective tissue disorders
DizzinessNervous system disorders
Abdominal painGastrointestinal disorders
Weight decreasedInvestigations
InsomniaPsychiatric disorders
Upper respiratory tract infectionInfections and infestations
Aspartate aminotransferase increasedInvestigations
NasopharyngitisInfections and infestations
HypertensionVascular disorders
Alanine aminotransferase increasedInvestigations
Musculoskeletal painMusculoskeletal and connective tissue disorders
HypothyroidismEndocrine disorders
Nasal congestionRespiratory, thoracic and mediastinal disorders
Dry skinSkin and subcutaneous tissue disorders
Influenza like illnessGeneral disorders
Urinary tract infectionInfections and infestations
PainGeneral disorders
AnxietyPsychiatric disorders
Dry mouthGastrointestinal disorders
HyperglycaemiaMetabolism and nutrition disorders

Most-reported serious reactions: Pleural effusion, Pneumonia, Squamous cell carcinoma, Dyspnoea, Cellulitis, Basal cell carcinoma, Pulmonary embolism, Pneumonitis.

Data from ClinicalTrials.gov NCT01295827 adverse events section.

Sponsor's own description

The present study has 5 parts. In Parts A and A1, the dose of intravenous (IV) pembrolizumab (MK-3475) will be escalated from 1 to 10 mg/kg to determine the maximum tolerated dose (MTD) and recommended Phase 2 dose (RP2D) for participants with a histologically- or cytologically-confirmed diagnosis of any type of carcinoma or melanoma (MEL) by evaluating the Dose Limiting Toxicities (DLTs). Following completion of the dose escalation, additional patients will be enrolled in Part A2 to further define pharmacokinetic characteristics. Part B of the study will investigate the safety, tolerability, and efficacy of pembrolizumab (2 mg/kg and 10 mg/kg) in participants with advanced or metastatic MEL and compare every 2 week dosing (Q2W) to every 3 week dosing (Q3W). Part C of the study will investigate the safety, tolerability, and efficacy of pembrolizumab administered at 10 mg/kg Q3W in participants with non-small cell lung carcinoma (NSCLC) that is locally advanced or metastatic. Part D of the study will investigate the low and high doses of study drug identified in Parts A and B (2 mg/kg and 10 mg/kg) administered Q3W in participants with advanced or metastatic MEL. Part E (closed with Amendment 7) was planned to investigate low, medium, and high doses of pembrolizumab in combination with standard chemotherapy in participants with locally advanced or metastatic NSCLC. Part F will investigate low and high doses of pembrolizumab (2 mg/kg and 10 mg/kg) administered Q2W or Q3W in treatment-naive and previously-treated participants with NSCLC with programmed cell death 1 ligand (PD-L1) gene expression. The primary hypotheses are the following: that pembrolizumab will have acceptable safety and tolerability; that pembrolizumab will show a clinically meaningful response rate (RR) or disease-control rate (DCR) in participants with melanoma (ipilimumab-refractory or not) and NSCLC, and that pembrolizumab will show a more clinically meaningful RR in participants with either cancer whose tumors express PD-L1.

Publications & conference data

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

  1. PD-1 blockade induces responses by inhibiting adaptive immune resistance.
    Tumeh PC, Harview CL, Yearley JH, Shintaku IP, et al · · 2014 · cited 5396× · PMID 25428505 · DOI 10.1038/nature13954
  2. Pembrolizumab for the treatment of non-small-cell lung cancer.
    Garon EB, Rizvi NA, Hui R, Leighl N, et al · · 2015 · cited 4857× · PMID 25891174 · DOI 10.1056/nejmoa1501824
  3. IFN-γ-related mRNA profile predicts clinical response to PD-1 blockade.
    Ayers M, Lunceford J, Nebozhyn M, Murphy E, et al · · 2017 · cited 2936× · PMID 28650338 · DOI 10.1172/jci91190
  4. Safety and tumor responses with lambrolizumab (anti-PD-1) in melanoma.
    Hamid O, Robert C, Daud A, Hodi FS, et al · · 2013 · cited 2609× · PMID 23724846 · DOI 10.1056/nejmoa1305133
  5. Pan-tumor genomic biomarkers for PD-1 checkpoint blockade-based immunotherapy.
    Cristescu R, Mogg R, Ayers M, Albright A, et al · · 2018 · cited 1784× · PMID 30309915 · DOI 10.1126/science.aar3593
  6. Anti-programmed-death-receptor-1 treatment with pembrolizumab in ipilimumab-refractory advanced melanoma: a randomised dose-comparison cohort of a phase 1 trial.
    Robert C, Ribas A, Wolchok JD, Hodi FS, et al · · 2014 · cited 1357× · PMID 25034862 · DOI 10.1016/s0140-6736(14)60958-2
  7. T-cell invigoration to tumour burden ratio associated with anti-PD-1 response.
    Huang AC, Postow MA, Orlowski RJ, Mick R, et al · · 2017 · cited 1350× · PMID 28397821 · DOI 10.1038/nature22079
  8. PD-1 and PD-L1 Checkpoint Signaling Inhibition for Cancer Immunotherapy: Mechanism, Combinations, and Clinical Outcome.
    Alsaab HO, Sau S, Alzhrani R, Tatiparti K, et al · · 2017 · cited 1206× · PMID 28878676 · DOI 10.3389/fphar.2017.00561

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