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Journal of Clinical Oncology, Vol 19, Issue 13 (July), 2001: 3267-3279
© 2001 American Society for Clinical Oncology

Phase I and Pharmacologic Study of OSI-774, an Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor, in Patients With Advanced Solid Malignancies

By Manuel Hidalgo, Lillian L. Siu, John Nemunaitis, Jinee Rizzo, Lisa A. Hammond, Chris Takimoto, S. Gail Eckhardt, Anthony Tolcher, Carolyn D. Britten, Louis Denis, Karen Ferrante, Daniel D. Von Hoff, Sandra Silberman, Eric K. Rowinsky

From the Institute for Drug Development, Cancer Therapy and Research Center, and the University of Texas Health Science Center at San Antonio, San Antonio, TX; U.S. Oncology, and Baylor University Medical Center, Dallas, TX; and Pfizer Pharmaceuticals, Inc, Groton, CT.

Address reprint requests to Manuel Hidalgo, MD, Department of Medicine, The University of Texas Health Science Center at San Antonio, 7703 Floyd Curl Dr, Mail Code 7884, San Antonio, TX 78229; email: manuelh{at}oncology.uthscsa.edu

PURPOSE: To assess the feasibility of administering OSI-774, to recommend a dose on a protracted, continuous daily schedule, to characterize its pharmacokinetic behavior, and to acquire preliminary evidence of anticancer activity.

PATIENTS AND METHODS: Patients with advanced solid malignancies were treated with escalating doses of OSI-774 in three study parts (A to C) to evaluate progressively longer treatment intervals. Part A patients received OSI-774 25 to 100 mg once daily, for 3 days each week, for 3 weeks every 4 weeks. Part B patients received OSI-774 doses ranging from 50 to 200 mg given once daily for 3 weeks every 4 weeks to establish the maximum tolerated dose (MTD). In part C, patients received this MTD on a continuous, uninterrupted schedule. The pharmacokinetics of OSI-774 and its O-demethylated metabolite, OSI-420, were characterized.

RESULTS: Forty patients received a total of 123 28-day courses of OSI-774. No severe toxicities precluded dose escalation of OSI-774 from 25 to 100 mg/d in part A. In part B, the incidence of severe diarrhea and/or cutaneous toxicity was unacceptably high at OSI-774 doses exceeding 150 mg/d. Uninterrupted, daily administration of OSI-774 150 mg/d represented the MTD on a protracted daily schedule. The pharmacokinetics of OSI-774 were dose independent; repetitive daily treatment did not result in drug accumulation (at 150 mg/d [average]: minimum steady-state plasma concentration, 1.20 ± 0.62 µg/mL; clearance rate, 6.33 ± 6.41 L/h; elimination half-life, 24.4 ± 14.6 hours; volume of distribution, 136. 4 ± 93.1 L; area under the plasma concentration-time curve for OSI-420 relative to OSI-774, 0.12 ± 0.12 µg/h/mL).

CONCLUSION: The recommended dose for disease-directed studies of OSI-774 administered orally on a daily, continuous, uninterrupted schedule is 150 mg/d. OSI-774 was well tolerated, and several patients with epidermoid malignancies demonstrated either antitumor activity or relatively long periods of stable disease. The precise contribution of OSI-774 to these effects is not known.

OSI-774 (OSI Pharmaceuticals, Uniondale, NY) was formerly known as CP-358,774 (Pfizer Global Research and Development, Groton, CT).

Presented in part at the Thirty-Fifth Annual Meeting of the American Society of Clinical Oncology, Atlanta, GA, May 15-19, 1999.


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E. Buck, A. Eyzaguirre, E. Brown, F. Petti, S. McCormack, J. D. Haley, K. K. Iwata, N. W. Gibson, and G. Griffin
Rapamycin synergizes with the epidermal growth factor receptor inhibitor erlotinib in non-small-cell lung, pancreatic, colon, and breast tumors.
Mol. Cancer Ther., November 1, 2006; 5(11): 2676 - 2684.
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T. Dragovich, S. McCoy, C. M. Fenoglio-Preiser, J. Wang, J. K. Benedetti, A. F. Baker, C. B. Hackett, S. G. Urba, K. S. Zaner, C. D. Blanke, et al.
Phase II Trial of Erlotinib in Gastroesophageal Junction and Gastric Adenocarcinomas: SWOG 0127
J. Clin. Oncol., October 20, 2006; 24(30): 4922 - 4927.
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E. Buck, A. Eyzaguirre, J. D. Haley, N. W. Gibson, P. Cagnoni, and K. K. Iwata
Inactivation of Akt by the epidermal growth factor receptor inhibitor erlotinib is mediated by HER-3 in pancreatic and colorectal tumor cell lines and contributes to erlotinib sensitivity.
Mol. Cancer Ther., August 1, 2006; 5(8): 2051 - 2059.
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S. S. Mitra and R. Simcock
Erlotinib Induced Skin Rash Spares Skin in Previous Radiotherapy Field
J. Clin. Oncol., June 1, 2006; 24(16): e28 - e29.
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K. L. Reckamp, K. Krysan, J. D. Morrow, G. L. Milne, R. A. Newman, C. Tucker, R. M. Elashoff, S. M. Dubinett, and R. A. Figlin
A phase I trial to determine the optimal biological dose of celecoxib when combined with erlotinib in advanced non-small cell lung cancer.
Clin. Cancer Res., June 1, 2006; 12(11): 3381 - 3388.
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C. Erlichman, M. Hidalgo, J. P. Boni, P. Martins, S. E. Quinn, C. Zacharchuk, P. Amorusi, A. A. Adjei, and E. K. Rowinsky
Phase I Study of EKB-569, an Irreversible Inhibitor of the Epidermal Growth Factor Receptor, in Patients With Advanced Solid Tumors
J. Clin. Oncol., May 20, 2006; 24(15): 2252 - 2260.
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S. Goodin
Erlotinib: optimizing therapy with predictors of response?
Clin. Cancer Res., May 15, 2006; 12(10): 2961 - 2963.
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E. Calvo and J. Baselga
Ethnic Differences in Response to Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors
J. Clin. Oncol., May 10, 2006; 24(14): 2158 - 2163.
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J. A. Meyerhardt, A. X. Zhu, P. C. Enzinger, D. P. Ryan, J. W. Clark, M. H. Kulke, C. C. Earle, M. Vincitore, A. Michelini, S. Sheehan, et al.
Phase II Study of Capecitabine, Oxaliplatin, and Erlotinib in Previously Treated Patients With Metastastic Colorectal Cancer
J. Clin. Oncol., April 20, 2006; 24(12): 1892 - 1897.
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J. Ling, K. A. Johnson, Z. Miao, A. Rakhit, M. P. Pantze, M. Hamilton, B. L. Lum, and C. Prakash
METABOLISM AND EXCRETION OF ERLOTINIB, A SMALL MOLECULE INHIBITOR OF EPIDERMAL GROWTH FACTOR RECEPTOR TYROSINE KINASE, IN HEALTHY MALE VOLUNTEERS
Drug Metab. Dispos., March 1, 2006; 34(3): 420 - 426.
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P. Frohna, J. Lu, S. Eppler, M. Hamilton, J. Wolf, A. Rakhit, J. Ling, S. R. Kenkare-Mitra, and B. L. Lum
Evaluation of the absolute oral bioavailability and bioequivalence of erlotinib, an inhibitor of the epidermal growth factor receptor tyrosine kinase, in a randomized, crossover study in healthy subjects.
J. Clin. Pharmacol., March 1, 2006; 46(3): 282 - 290.
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M. D. Prados, K. R. Lamborn, S. Chang, E. Burton, N. Butowski, M. Malec, A. Kapadia, J. Rabbitt, M. S. Page, A. Fedoroff, et al.
Phase 1 study of erlotinib HCl alone and combined with temozolomide in patients with stable or recurrent malignant glioma
Neuro-oncol, January 1, 2006; 8(1): 67 - 78.
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H. T. Cohen and F. J. McGovern
Renal-Cell Carcinoma
N. Engl. J. Med., December 8, 2005; 353(23): 2477 - 2490.
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J. D. Hainsworth, J. A. Sosman, D. R. Spigel, D. L. Edwards, C. Baughman, and A. Greco
Treatment of Metastatic Renal Cell Carcinoma With a Combination of Bevacizumab and Erlotinib
J. Clin. Oncol., November 1, 2005; 23(31): 7889 - 7896.
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D. H. Garfield
Modern Treatment of Lung Cancer: CASE 2. Response to Erlotinib After Failure of Gefitinib in a Patient With Advanced Non-Small-Cell Lung Carcinoma
J. Clin. Oncol., October 20, 2005; 23(30): 7738 - 7740.
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R. Hoekstra, H. Dumez, F. A.L.M. Eskens, A. van der Gaast, A. S.T. Planting, G. de Heus, K. C. Sizer, C. Ravera, S. Vaidyanathan, C. Bucana, et al.
Phase I and Pharmacologic Study of PKI166, an Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor, in Patients with Advanced Solid Malignancies
Clin. Cancer Res., October 1, 2005; 11(19): 6908 - 6915.
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R. S. Herbst, D. Prager, R. Hermann, L. Fehrenbacher, B. E. Johnson, A. Sandler, M. G. Kris, H. T. Tran, P. Klein, X. Li, et al.
TRIBUTE: A Phase III Trial of Erlotinib Hydrochloride (OSI-774) Combined With Carboplatin and Paclitaxel Chemotherapy in Advanced Non-Small-Cell Lung Cancer
J. Clin. Oncol., September 1, 2005; 23(25): 5892 - 5899.
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M. S. Choe, X. Zhang, H. J. C. Shin, D. M. Shin, and Z. Chen
Interaction between epidermal growth factor receptor- and cyclooxygenase 2-mediated pathways and its implications for the chemoprevention of head and neck cancer
Mol. Cancer Ther., September 1, 2005; 4(9): 1448 - 1455.
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S. Segaert and E. Van Cutsem
Clinical signs, pathophysiology and management of skin toxicity during therapy with epidermal growth factor receptor inhibitors
Ann. Onc., September 1, 2005; 16(9): 1425 - 1433.
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S. X. Yang, R. M. Simon, A. R. Tan, D. Nguyen, and S. M. Swain
Gene Expression Patterns and Profile Changes Pre- and Post-Erlotinib Treatment in Patients with Metastatic Breast Cancer
Clin. Cancer Res., September 1, 2005; 11(17): 6226 - 6232.
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 The OncologistHome page
W. S. Siegel-Lakhai, J. H. Beijnen, and J. H.M. Schellens
Current Knowledge and Future Directions of the Selective Epidermal Growth Factor Receptor Inhibitors Erlotinib (Tarceva(R)) and Gefitinib (Iressa(R))
Oncologist, September 1, 2005; 10(8): 579 - 589.
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H. A. Burris III, H. I. Hurwitz, E. C. Dees, A. Dowlati, K. L. Blackwell, B. O'Neil, P. K. Marcom, M. J. Ellis, B. Overmoyer, S. F. Jones, et al.
Phase I Safety, Pharmacokinetics, and Clinical Activity Study of Lapatinib (GW572016), a Reversible Dual Inhibitor of Epidermal Growth Factor Receptor Tyrosine Kinases, in Heavily Pretreated Patients With Metastatic Carcinomas
J. Clin. Oncol., August 10, 2005; 23(23): 5305 - 5313.
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P. M. LoRusso, A. A. Adjei, M. Varterasian, S. Gadgeel, J. Reid, D. Y. Mitchell, L. Hanson, P. DeLuca, L. Bruzek, J. Piens, et al.
Phase I and Pharmacodynamic Study of the Oral MEK Inhibitor CI-1040 in Patients With Advanced Malignancies
J. Clin. Oncol., August 10, 2005; 23(23): 5281 - 5293.
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R. Perez-Soler and L. Saltz
Cutaneous Adverse Effects With HER1/EGFR-Targeted Agents: Is There a Silver Lining?
J. Clin. Oncol., August 1, 2005; 23(22): 5235 - 5246.
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F. R. Luo, Z. Yang, H. Dong, A. Camuso, K. McGlinchey, K. Fager, C. Flefleh, D. Kan, I. Inigo, S. Castaneda, et al.
Prediction of Active Drug Plasma Concentrations Achieved in Cancer Patients by Pharmacodynamic Biomarkers Identified from the Geo Human Colon Carcinoma Xenograft Model
Clin. Cancer Res., August 1, 2005; 11(15): 5558 - 5565.
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 The OncologistHome page
M. H. Cohen, J. R. Johnson, Y.-F. Chen, R. Sridhara, and R. Pazdur
FDA Drug Approval Summary: Erlotinib (Tarceva(R)) Tablets
Oncologist, August 1, 2005; 10(7): 461 - 466.
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J. Nemunaitis, I. Eiseman, C. Cunningham, N. Senzer, A. Williams, P. F. Lenehan, S. C. Olson, P. Bycott, M. Schlicht, R. Zentgraff, et al.
Phase 1 Clinical and Pharmacokinetics Evaluation of Oral CI-1033 in Patients with Refractory Cancer
Clin. Cancer Res., May 15, 2005; 11(10): 3846 - 3853.
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R. Perez-Soler, J. P. Delord, A. Halpern, K. Kelly, J. Krueger, B. M. Sureda, J. von Pawel, J. Temel, S. Siena, D. Soulieres, et al.
HER1/EGFR Inhibitor-Associated Rash: Future Directions for Management and Investigation Outcomes from the HER1/EGFR Inhibitor Rash Management Forum
Oncologist, May 1, 2005; 10(5): 345 - 356.
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P. Chinnaiyan, S. Huang, G. Vallabhaneni, E. Armstrong, S. Varambally, S. A. Tomlins, A. M. Chinnaiyan, and P. M. Harari
Mechanisms of Enhanced Radiation Response following Epidermal Growth Factor Receptor Signaling Inhibition by Erlotinib (Tarceva)
Cancer Res., April 15, 2005; 65(8): 3328 - 3335.
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D. B. Agus, M. S. Gordon, C. Taylor, R. B. Natale, B. Karlan, D. S. Mendelson, M. F. Press, D. E. Allison, M. X. Sliwkowski, G. Lieberman, et al.
Phase I Clinical Study of Pertuzumab, a Novel HER Dimerization Inhibitor, in Patients With Advanced Cancer
J. Clin. Oncol., April 10, 2005; 23(11): 2534 - 2543.
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J. Baselga and C. L. Arteaga
Critical Update and Emerging Trends in Epidermal Growth Factor Receptor Targeting in Cancer
J. Clin. Oncol., April 10, 2005; 23(11): 2445 - 2459.
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R. S. Herbst, D. H. Johnson, E. Mininberg, D. P. Carbone, T. Henderson, E. S. Kim, G. Blumenschein Jr, J. J. Lee, D. D. Liu, M. T. Truong, et al.
Phase I/II Trial Evaluating the Anti-Vascular Endothelial Growth Factor Monoclonal Antibody Bevacizumab in Combination With the HER-1/Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor Erlotinib for Patients With Recurrent Non-Small-Cell Lung Cancer
J. Clin. Oncol., April 10, 2005; 23(11): 2544 - 2555.
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W. Pao and V. A. Miller
Epidermal Growth Factor Receptor Mutations, Small-Molecule Kinase Inhibitors, and Non-Small-Cell Lung Cancer: Current Knowledge and Future Directions
J. Clin. Oncol., April 10, 2005; 23(11): 2556 - 2568.
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D. McKillop, E. A. Partridge, J. V. Kemp, M. P. Spence, J. Kendrew, S. Barnett, P. G. Wood, P. B. Giles, A. B. Patterson, F. Bichat, et al.
Tumor penetration of gefitinib (Iressa), an epidermal growth factor receptor tyrosine kinase inhibitor
Mol. Cancer Ther., April 1, 2005; 4(4): 641 - 649.
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G. Giaccone
HER1/EGFR-targeted agents: predicting the future for patients with unpredictable outcomes to therapy
Ann. Onc., April 1, 2005; 16(4): 538 - 548.
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K. Y. Chung, J. Shia, N. E. Kemeny, M. Shah, G. K. Schwartz, A. Tse, A. Hamilton, D. Pan, D. Schrag, L. Schwartz, et al.
Cetuximab Shows Activity in Colorectal Cancer Patients With Tumors That Do Not Express the Epidermal Growth Factor Receptor by Immunohistochemistry
J. Clin. Oncol., March 20, 2005; 23(9): 1803 - 1810.
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I. Shin, J. Rotty, F. Y. Wu, and C. L. Arteaga
Phosphorylation of p27Kip1 at Thr-157 Interferes with Its Association with Importin {alpha} during G1 and Prevents Nuclear Re-entry
J. Biol. Chem., February 18, 2005; 280(7): 6055 - 6063.
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Q. Dai, Y.-H. Ling, M. Lia, Y.-Y. Zou, G. Kroog, K. K. Iwata, and R. Perez-Soler
Enhanced Sensitivity to the HER1/Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor Erlotinib Hydrochloride in Chemotherapy-Resistant Tumor Cell Lines
Clin. Cancer Res., February 15, 2005; 11(4): 1572 - 1578.
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J. P. Spano, R. Fagard, J.-C. Soria, O. Rixe, D. Khayat, and G. Milano
Epidermal growth factor receptor signaling in colorectal cancer: preclinical data and therapeutic perspectives
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