A first-in-human phase 1 dose escalation study of spartalizumab (PDR001), an anti–PD-1 antibody, in patients with advanced solid tumors

Background Spartalizumab is a humanized IgG4κ monoclonal antibody that binds programmed death-1 (PD-1) and blocks its interaction with PD-L1 and PD-L2. This phase 1/2 study was designed to assess the safety, pharmacokinetics, and preliminary efficacy of spartalizumab in patients with advanced or met...

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Main Authors: Hans Gelderblom, Patrick M Forde, Aung Naing, Matthew Taylor, Jennifer Mataraza, Marcus O Butler, Todd M Bauer, Justin F Gainor, Chia-Chi Lin, Sunil Sharma, Maria Ochoa de Olza, Andrea Varga, Jan H M Schellens, Hongqian Wu, Haiying Sun, Antonio P Silva, Jason Faris, Scott Cameron
Format: Article
Language:English
Published: BMJ Publishing Group 2020-05-01
Series:Journal for ImmunoTherapy of Cancer
Online Access:https://jitc.bmj.com/content/8/1/e000530.full
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author Hans Gelderblom
Patrick M Forde
Aung Naing
Matthew Taylor
Jennifer Mataraza
Marcus O Butler
Todd M Bauer
Justin F Gainor
Chia-Chi Lin
Sunil Sharma
Maria Ochoa de Olza
Andrea Varga
Jan H M Schellens
Hongqian Wu
Haiying Sun
Antonio P Silva
Jason Faris
Scott Cameron
author_facet Hans Gelderblom
Patrick M Forde
Aung Naing
Matthew Taylor
Jennifer Mataraza
Marcus O Butler
Todd M Bauer
Justin F Gainor
Chia-Chi Lin
Sunil Sharma
Maria Ochoa de Olza
Andrea Varga
Jan H M Schellens
Hongqian Wu
Haiying Sun
Antonio P Silva
Jason Faris
Scott Cameron
author_sort Hans Gelderblom
collection DOAJ
description Background Spartalizumab is a humanized IgG4κ monoclonal antibody that binds programmed death-1 (PD-1) and blocks its interaction with PD-L1 and PD-L2. This phase 1/2 study was designed to assess the safety, pharmacokinetics, and preliminary efficacy of spartalizumab in patients with advanced or metastatic solid tumors.Methods In the phase 1 part of the study, 58 patients received spartalizumab, intravenously, at doses of 1, 3, or 10 mg/kg, administered every 2 weeks (Q2W), or 3 or 5 mg/kg every 4 weeks (Q4W).Results Patients had a wide range of tumor types, most commonly sarcoma (28%) and metastatic renal cell carcinoma (10%); other tumor types were reported in ≤3 patients each. Most patients (93%) had received prior antineoplastic therapy (median three prior lines) and two-thirds of the population had tumor biopsies negative for PD-L1 expression at baseline. The maximum tolerated dose was not reached. The recommended phase 2 doses were selected as 400 mg Q4W or 300 mg Q3W. No dose-limiting toxicities were observed, and adverse events included those typical of other PD-1 antibodies. The most common treatment-related adverse events of any grade were fatigue (22%), diarrhea (17%), pruritus (14%), hypothyroidism (10%), and nausea (10%). Partial responses occurred in two patients (response rate 3.4%); one with atypical carcinoid tumor of the lung and one with anal cancer. Paired tumor biopsies from patients taken at baseline and on treatment suggested an on-treatment increase in CD8+ lymphocyte infiltration in patients with clinical benefit.Conclusions Spartalizumab was well tolerated at all doses tested in patients with previously treated advanced solid tumors. On-treatment immune activation was seen in tumor biopsies; however, limited clinical activity was reported in this heavily pretreated, heterogeneous population. The phase 2 part of this study is ongoing in select tumor types.Trial registration number NCT02404441.
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spelling doaj-art-d6d1da80e61d43f995ed1d456acbc0932024-11-09T09:10:08ZengBMJ Publishing GroupJournal for ImmunoTherapy of Cancer2051-14262020-05-018110.1136/jitc-2020-000530A first-in-human phase 1 dose escalation study of spartalizumab (PDR001), an anti–PD-1 antibody, in patients with advanced solid tumorsHans Gelderblom0Patrick M Forde1Aung Naing2Matthew Taylor3Jennifer Mataraza4Marcus O Butler5Todd M Bauer6Justin F Gainor7Chia-Chi Lin8Sunil Sharma9Maria Ochoa de Olza10Andrea Varga11Jan H M Schellens12Hongqian Wu13Haiying Sun14Antonio P Silva15Jason Faris16Scott Cameron17Department of Medical Oncology, Leiden University Medical Center, Leiden, The NetherlandsDepartment of Oncology, The Sidney Kimmel Comprehensive Cancer Center and the Bloomberg–Kimmel Institute for Cancer Immunotherapy, Johns Hopkins University, Baltimore, Maryland, USA14 Department of Investigational Cancer Therapeutics, Division of Cancer Medicine, The University of Texas MD Anderson Cancer Center, Houston, Texas, USA11 Providence Cancer Center, Portland, Oregon, USAOncology Translational Research, Novartis Institutes for BioMedical Research Inc, Cambridge, Massachusetts, USAPrincess Margaret Hospital Cancer Centre, Toronto, Ontario, CanadaSarah Cannon Research Institute, Nashville, Tennessee, USAMassachusetts General Hospital, Boston, Massachusetts, USA6 National Taiwan University Hospital, Taipei, Taiwan2Stingray Therapeutics, Houston, TX1 Immuno-oncology Service, Department of Oncology, CHUV, Lausanne, Vaud, SwitzerlandPalliative Care Unit, Gustave Roussy Institute, Villejuif, France11 Utrecht University, Utrecht, The Netherlands12 Novartis Pharmaceuticals Corporation, East Hanover, New Jersey, USA12 Novartis Pharmaceuticals Corporation, East Hanover, New Jersey, USA13 Novartis Institutes for BioMedical Research, Basel, Switzerland14 Novartis Institutes for BioMedical Research, Cambridge, Massachusetts, USA14 Novartis Institutes for BioMedical Research, Cambridge, Massachusetts, USABackground Spartalizumab is a humanized IgG4κ monoclonal antibody that binds programmed death-1 (PD-1) and blocks its interaction with PD-L1 and PD-L2. This phase 1/2 study was designed to assess the safety, pharmacokinetics, and preliminary efficacy of spartalizumab in patients with advanced or metastatic solid tumors.Methods In the phase 1 part of the study, 58 patients received spartalizumab, intravenously, at doses of 1, 3, or 10 mg/kg, administered every 2 weeks (Q2W), or 3 or 5 mg/kg every 4 weeks (Q4W).Results Patients had a wide range of tumor types, most commonly sarcoma (28%) and metastatic renal cell carcinoma (10%); other tumor types were reported in ≤3 patients each. Most patients (93%) had received prior antineoplastic therapy (median three prior lines) and two-thirds of the population had tumor biopsies negative for PD-L1 expression at baseline. The maximum tolerated dose was not reached. The recommended phase 2 doses were selected as 400 mg Q4W or 300 mg Q3W. No dose-limiting toxicities were observed, and adverse events included those typical of other PD-1 antibodies. The most common treatment-related adverse events of any grade were fatigue (22%), diarrhea (17%), pruritus (14%), hypothyroidism (10%), and nausea (10%). Partial responses occurred in two patients (response rate 3.4%); one with atypical carcinoid tumor of the lung and one with anal cancer. Paired tumor biopsies from patients taken at baseline and on treatment suggested an on-treatment increase in CD8+ lymphocyte infiltration in patients with clinical benefit.Conclusions Spartalizumab was well tolerated at all doses tested in patients with previously treated advanced solid tumors. On-treatment immune activation was seen in tumor biopsies; however, limited clinical activity was reported in this heavily pretreated, heterogeneous population. The phase 2 part of this study is ongoing in select tumor types.Trial registration number NCT02404441.https://jitc.bmj.com/content/8/1/e000530.full
spellingShingle Hans Gelderblom
Patrick M Forde
Aung Naing
Matthew Taylor
Jennifer Mataraza
Marcus O Butler
Todd M Bauer
Justin F Gainor
Chia-Chi Lin
Sunil Sharma
Maria Ochoa de Olza
Andrea Varga
Jan H M Schellens
Hongqian Wu
Haiying Sun
Antonio P Silva
Jason Faris
Scott Cameron
A first-in-human phase 1 dose escalation study of spartalizumab (PDR001), an anti–PD-1 antibody, in patients with advanced solid tumors
Journal for ImmunoTherapy of Cancer
title A first-in-human phase 1 dose escalation study of spartalizumab (PDR001), an anti–PD-1 antibody, in patients with advanced solid tumors
title_full A first-in-human phase 1 dose escalation study of spartalizumab (PDR001), an anti–PD-1 antibody, in patients with advanced solid tumors
title_fullStr A first-in-human phase 1 dose escalation study of spartalizumab (PDR001), an anti–PD-1 antibody, in patients with advanced solid tumors
title_full_unstemmed A first-in-human phase 1 dose escalation study of spartalizumab (PDR001), an anti–PD-1 antibody, in patients with advanced solid tumors
title_short A first-in-human phase 1 dose escalation study of spartalizumab (PDR001), an anti–PD-1 antibody, in patients with advanced solid tumors
title_sort first in human phase 1 dose escalation study of spartalizumab pdr001 an anti pd 1 antibody in patients with advanced solid tumors
url https://jitc.bmj.com/content/8/1/e000530.full
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