Phase I Dose-Escalation Study of the Pan-HER Inhibitor, PF299804, in Patients with Advanced Malignant Solid Tumors

Jänne, Pasi A.; Boss, David S.; Camidge, D. Ross; Britten, Carolyn D.; Engelman, Jeffrey A.; Garon, Edward B.; Guo, Feng; Wong, Steven; Liang, Jane; Letrent, Stephen; Millham, Robert; Taylor, Ian; Eckhardt, S. Gail; Schellens, Jan H.M.

doi:10.1158/1078-0432.ccr-10-1220

Cited by 181Lung Cancer Treatments and MutationsHER2/EGFR in Cancer ResearchCancer Mechanisms and Therapy

Phase I Dose-Escalation Study of the Pan-HER Inhibitor, PF299804, in Patients with Advanced Malignant Solid Tumors

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Jänne, Pasi A., Boss, David S., Camidge, D. Ross, Britten, Carolyn D., Engelman, Jeffrey A., Garon, Edward B., Guo, Feng, Wong, Steven +6 more·2011·Clinical Cancer Research

DOI 10.1158/1078-0432.ccr-10-1220PMC PMC3048920

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Abstract

Purpose: PF299804 is a potent, orally available, irreversible inhibitor of tyrosine kinase human epidermal growth factor receptors (HER) 1 (EGFR), HER2, and HER4. This first-in-human study investigated the safety, tolerability, pharmacokinetics, and pharmacodynamics of PF299804 in patients with advanced solid malignancies. Experimental Design: PF299804 was administered once daily continuously (schedule A) and intermittently (schedule B). Dose escalation proceeded until intolerable toxicities occurred. Skin biopsies were taken predose and after 14 days of treatment to establish a pharmacokinetic/pharmacodynamic relationship. Tumor response was measured once every 2 cycles. Efficacy was correlated with tumor genotypes in non–small cell lung cancer (NSCLC) patients. Results: 121 patients were included (111 in schedule A, 10 in schedule B). The maximum tolerated dose (MTD) was 45 mg/d. Dose-limiting toxicities included stomatitis and skin toxicities. Most adverse events were mild and comprised skin toxicities, fatigue, and gastrointestinal side-effects including diarrhea, nausea, and vomiting. Pharmacokinetic analyses revealed dose-dependent increases in PF299804 exposure associated with target inhibition in skin biopsy samples. Fifty-seven patients with non–small cell lung cancer (NSCLC) were treated in this study. Four patients, all previously treated with gefitinib or erlotinib (2 with exon 19 deletions, 1 with exon 20 insertion, 1 mutational status unknown), had a partial response to PF299804. Conclusions: The MTD of PF299804 is 45 mg/d. Both continuous and intermittent treatment schedules were well tolerated, and encouraging signs of antitumor activity were observed in gefitinib/erlotinib treated NSCLC patients. Clin Cancer Res; 17(5); 1131–9. ©2011 AACR.

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Clinical testing of afatinib, neratinib, and dacomitinib achieved overall response rates of 8.7%, 9.5%, and 12%, respectively, for patients harboring EGFR or HER2 exon 20 mutations.
“In concordance with this, clinical testing of afatinib, neratinib, and dacomitinib achieved overall response rates of 8.7%, 9.5%, and 12%, respectively, for patients harboring EGFR or HER2 exon 20 mutations25,42,46,47.”
From Mechanisms and clinical activity of an EGFR and HER2 exon 20–selective kinase inhibitor in non–small cell lung cancer (2018) · cites this paper as [42]
Other first-, second-, and third-generation TKIs had IC50 values above clinically achievable plasma concentrations previously observed in patients.
“By contrast, other first-, second-, and third-generation TKIs had IC50 values that were above the clinically achievable plasma concentrations previously observed in patients31,41,42,43,44,45.”
From Mechanisms and clinical activity of an EGFR and HER2 exon 20–selective kinase inhibitor in non–small cell lung cancer (2018) · cites this paper as [42]
NSCLC tumors carrying EGFR or HER2 exon 20 insertion mutations rarely show clinical responses to dacomitinib or afatinib.
“Non-small cell lung cancer (NSCLC) patients with tumors harboring these mutations seldom achieve clinical responses to dacomitinib and afatinib, two covalent quinazoline-based inhibitors of EGFR or HER2, respectively.”
From Response Heterogeneity of EGFR and HER2 Exon 20 Insertions to Covalent EGFR and HER2 Inhibitors (2017) · cites this paper as [25]
One patient with the D770delinsGY EGFR mutation showed a partial response to dacomitinib.
“Some of these patients were enrolled in clinical trials of dacomitinib treatment, and one patient with D770delinsGY showed partial response (25).”
From Response Heterogeneity of EGFR and HER2 Exon 20 Insertions to Covalent EGFR and HER2 Inhibitors (2017) · cites this paper as [25]
In the phase I dacomitinib study, 1 of 6 patients with EGFR exon 20 insertions had a sustained partial response.
“In the phase I study of dacomitinib, 6 patients with EGFR exon 20 insertions were treated and 1 of 6 patients had a sustained PR (25).”
From Response Heterogeneity of EGFR and HER2 Exon 20 Insertions to Covalent EGFR and HER2 Inhibitors (2017) · cites this paper as [25]

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Authors: Jänne, P. A., Boss, D. S., Camidge, D. R., Britten, C. D., Engelman, J. A., Garon, E. B., Guo, F., Wong, S., Liang, J., Letrent, S., Millham, R., Taylor, I., Eckhardt, S. G., & Schellens, J. H. M.
Affiliations: Authors' Affiliations: 1Dana Farber Cancer Institute and 2Massachusetts General Hospital Cancer Center, Boston, Massachusetts; 3Netherlands Cancer Institute, Division of Clinical Pharmacology, Amsterdam, The Netherlands; 4University of Colorado, Denver, Aurora, Colorado; 5University of California Los Angeles, UCLA Medical Center, Los Angeles, California; 6Clinical Pharmacology and Pharmacometrics, Pfizer (China) Research and Development Center, Shanghai, P.R. China; 7Pfizer Oncology, New London, Connecticut; 8Clinical Development and Medical Affairs, Pfizer Oncology, San Diego, California; and 9Faculty of Pharmaceutical Sciences, Division of Drug Toxicology, University Utrecht, Utrecht, the Netherlands
University of California, Los Angeles (US)
ORCID: Camidge, D. Ross
Engelman, Jeffrey A.
Garon, Edward B.
Schellens, Jan H.M.
Venue: Clinical Cancer Research
Publisher: American Association for Cancer Research (AACR)
Published: 2011-03-01
Volume: 17
Issue: 5
Pages: 1131-1139
ISSN: 1078-0432 (ISSN-L)
1557-3265
DOI: 10.1158/1078-0432.ccr-10-1220
PMC: PMC3048920
OpenAlex: W2161152839
Cited by: 181
References: 23
Citations by year: 2026: 3 · 2025: 2 · 2024: 2 · 2023: 6 · 2022: 12 · 2021: 13 · 2020: 10 · 2019: 10 · 2018: 14 · 2017: 12 · 2016: 14 · 2015: 18 · 2014: 18 · 2013: 22 · 2012: 18
FWCI: 17.54
Type: journal article
Language: en
Open access: green
www.ncbi.nlm.nih.gov
Locations: Clinical Cancer Research (publishedVersion)
PubMed (publishedVersion)
Europe PMC (PubMed Central) (acceptedVersion)
PubMed Central (acceptedVersion)
Funders: Pfizer
National Institutes of Health
National Cancer Institute (P50CA090578, R01CA135257)
Topics: Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Lung Cancer Treatments and Mutations
Health Sciences › Medicine › Oncology › HER2/EGFR in Cancer Research
Health Sciences › Medicine › Pathology and Forensic Medicine › Cancer Mechanisms and Therapy
Keywords: pan-HER inhibitor, EGFR, HER2, ErbB4, tyrosine kinase inhibitors, dose escalation, maximum tolerated dose, non-small cell lung cancer, stomatitis, skin toxicity, pharmacokinetics, pharmacodynamics, exon 19 deletion, exon 20 insertion, anticancer activity
MeSH terms: Erlotinib Hydrochloride, Gefitinib, Adult, Aged, Antineoplastic Agents, Carcinoma, Non-Small-Cell Lung, Female, Genotype, Heptanoic Acids, Humans, Lung Neoplasms, Male, Middle Aged, Mutation, Protein-Tyrosine Kinases, Pyrazoles, Quinazolines, Biomarkers, Tumor, Signal Transduction, Treatment Outcome, Erb-b2 Receptor Tyrosine Kinases, Maximum Tolerated Dose, ErbB Receptors, Receptor, ErbB-4

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Phase I Dose-Escalation Study of the Pan-HER Inhibitor, PF299804, in Patients with Advanced Malignant Solid Tumors

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