A phase i study of AST1306, a novel irreversible EGFR and HER2 kinase inhibitor, in patients with advanced solid tumors

Journal of Hematology and Oncology

Volumn 7, Issue 1, 2014, Pages

  Zhang, Jian ^a,b   Cao, Junning ^a,b   Li, Jin ^a,b   Zhang, Yifan ^c   Chen, Zhiyu ^a,b   Peng, Wei ^a,b   Sun, Si ^a,b   Zhao, Naiqing ^b   Wang, Jiachen ^a,b   Zhong, Dafang ^c   Zhang, Xiaofang ^d   Zhang, Jing ^d  

^a FUDAN UNIVERSITY SHANGHAI CANCER CENTER   (China)

^b FUDAN UNIVERSITY   (China)

^c SHANGHAI INSTITUTE OF MATERIA MEDICA   (China)

^d Department of Biostatistics School of Public Health Fudan University ^*  (China)

Author keywords

AST1306; ErbB family; Irreversible tyrosine kinase inhibitor; Phase I

Indexed keywords

ALANINE AMINOTRANSFERASE; ANTINEOPLASTIC AGENT; AST 1306; UNCLASSIFIED DRUG; ACRYLAMIDE DERIVATIVE; EGFR PROTEIN, HUMAN; EPIDERMAL GROWTH FACTOR RECEPTOR; EPIDERMAL GROWTH FACTOR RECEPTOR 2; ERBB2 PROTEIN, HUMAN; PROTEIN KINASE INHIBITOR; QUINAZOLINE DERIVATIVE;

ABDOMINAL PAIN; ADULT; ADVANCED CANCER; AGED; ALANINE AMINOTRANSFERASE BLOOD LEVEL; ANEMIA; ANOREXIA; ANTINEOPLASTIC ACTIVITY; AREA UNDER THE CURVE; ARTICLE; BLEEDING; BREAST CANCER; COHORT ANALYSIS; CONTINUOUS INFUSION; CROSSOVER PROCEDURE; DIARRHEA; DISEASE DURATION; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG DOSE ESCALATION; DRUG DOSE REDUCTION; DRUG ERUPTION; DRUG SAFETY; DRUG TOLERABILITY; FATIGUE; FEBRILE NEUTROPENIA; FEMALE; HAND FOOT SYNDROME; HUMAN; HYPOKALEMIA; LUNG CANCER; MAJOR CLINICAL STUDY; MALE; MAXIMUM PLASMA CONCENTRATION; MAXIMUM TOLERATED DOSE; NAUSEA; NEUTROPENIA; PHASE 1 CLINICAL TRIAL; PRIMARY TUMOR; PROTEINURIA; RECOMMENDED DRUG DOSE; SIDE EFFECT; SOLID TUMOR; STOMACH CANCER; THROMBOCYTOPENIA; TIME TO MAXIMUM PLASMA CONCENTRATION; TREATMENT RESPONSE; VOMITING; ADOLESCENT; ANTAGONISTS AND INHIBITORS; CLINICAL TRIAL; CONTROLLED STUDY; DOSE RESPONSE; ENZYMOLOGY; METABOLISM; MIDDLE AGED; NEOPLASMS; RANDOMIZED CONTROLLED TRIAL; TREATMENT OUTCOME; YOUNG ADULT;

ACRYLAMIDES; ADOLESCENT; ADULT; AGED; DOSE-RESPONSE RELATIONSHIP, DRUG; FEMALE; HUMANS; MALE; MIDDLE AGED; NEOPLASMS; PROTEIN KINASE INHIBITORS; QUINAZOLINES; RECEPTOR, EPIDERMAL GROWTH FACTOR; RECEPTOR, ERBB-2; TREATMENT OUTCOME; YOUNG ADULT;

EID: 84907444509     PISSN: None     EISSN: 17568722     Source Type: Journal    
DOI: 10.1186/1756-8722-7-22     Document Type: Article

References (28)

1. Untangling the ErbB signalling network. Yarden Y, Sliwkowski MX, Nat Rev Mol Cell Biol 2001 2 127 137 10.1038/35052073 11252954
2. Targeting the ERBB family in cancer: couples therapy. Tebbutt N, Pedersen MW, Johns TG, Nat Rev Cancer 2013 13 663 673 10.1038/nrc3559 23949426
3. Mechanisms of acquired resistance to epidermal growth factor receptor tyrosine kinase inhibitors in non-small cell lung cancer. Engelman JA, Janne PA, Clin Cancer Res 2008 14 2895 2899 10.1158/1078-0432.CCR-07-2248 18483355
4. Gefitinib or carboplatin-paclitaxel in pulmonary adenocarcinoma. Mok TS, Wu YL, Thongprasert S, Yang CH, Chu DT, Saijo N, Sunpaweravong P, Han B, Margono B, Ichinose Y, Nishiwaki Y, Ohe Y, Yang JJ, Chewaskulyong B, Jiang H, Duffield EL, Watkins CL, Armour AA, Fukuoka M, N Engl J Med 2009 361 947 957 10.1056/NEJMoa0810699 19692680
5. A phase II study of afatinib (BIBW 2992), an irreversible ErbB family blocker, in patients with HER2-positive metastatic breast cancer progressing after trastuzumab. Lin NU, Winer EP, Wheatley D, Carey LA, Houston S, Mendelson D, Munster P, Frakes L, Kelly S, Garcia AA, Cleator S, Uttenreuther-Fischer M, Jones H, Wind S, Vinisko R, Hickish T, Breast Cancer Res Treat 2012 133 1057 1065 10.1007/s10549-012-2003-y 22418700
6. AST1306, a novel irreversible inhibitor of the epidermal growth factor receptor 1 and 2, exhibits antitumor activity both in vitro and in vivo. Xie H, Lin L, Tong L, Jiang Y, Zheng M, Chen Z, Jiang X, Zhang X, Ren X, Qu W, Yang Y, Wan H, Chen Y, Zuo J, Jiang H, Geng M, Ding J, PLoS One 2011 6 21487 10.1371/journal.pone.0021487 21789172
7. BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models. Li D, Ambrogio L, Shimamura T, Kubo S, Takahashi M, Chirieac LR, Padera RF, Shapiro GI, Baum A, Himmelsbach F, Rettig WJ, Meyerson M, Solca F, Greulich H, Wong KK, Oncogene 2008 27 4702 4711 10.1038/onc.2008.109 18408761
8. EGFR mutation and resistance of non-small-cell lung cancer to gefitinib. Kobayashi S, Boggon TJ, Dayaram T, Janne PA, Kocher O, Meyerson M, Johnson BE, Eck MJ, Tenen DG, Halmos B, N Engl J Med 2005 352 786 792 10.1056/NEJMoa044238 15728811
9. Acquired resistance of lung adenocarcinomas to gefitinib or erlotinib is associated with a second mutation in the EGFR kinase domain. Pao W, Miller VA, Politi KA, Riely GJ, Somwar R, Zakowski MF, Kris MG, Varmus H, PLoS Med 2005 2 73 10.1371/journal.pmed.0020073 15737014
10. Novel D761Y and common secondary T790M mutations in epidermal growth factor receptor-mutant lung adenocarcinomas with acquired resistance to kinase inhibitors. Balak MN, Gong Y, Riely GJ, Somwar R, Li AR, Zakowski MF, Chiang A, Yang G, Ouerfelli O, Kris MG, Ladanyi M, Miller VA, Pao W, Clin Cancer Res 2006 12 6494 6501 10.1158/1078-0432.CCR-06-1570 17085664
11. Can rash associated with HER1/EGFR inhibition be used as a marker of treatment outcome? Perez-Soler R, Oncology (Williston Park) 2003 17 23 28
12. Multi-institutional randomized phase II trial of gefitinib for previously treated patients with advanced non-small-cell lung cancer (The IDEAL 1 Trial) [corrected]. Fukuoka M, Yano S, Giaccone G, Tamura T, Nakagawa K, Douillard JY, Nishiwaki Y, Vansteenkiste J, Kudoh S, Rischin D, Eek R, Horai T, Noda K, Takata I, Smit E, Averbuch S, Macleod A, Feyereislova A, Dong RP, Baselga J, J Clin Oncol 2003 21 2237 2246 10.1200/JCO.2003.10.038 12748244
13. Efficacy of gefitinib, an inhibitor of the epidermal growth factor receptor tyrosine kinase, in symptomatic patients with non-small cell lung cancer: a randomized trial. Kris MG, Natale RB, Herbst RS, Lynch TJ, Prager D, Belani CP, Schiller JH, Kelly K, Spiridonidis H, Sandler A, Albain KS, Cella D, Wolf MK, Averbuch SD, Ochs JJ, Kay AC, JAMA 2003 290 2149 2158 10.1001/jama.290.16.2149 14570950
14. Phase I, dose-finding study of AZD8931, an inhibitor of EGFR (erbB1), HER2 (erbB2) and HER3 (erbB3) signaling, in patients with advanced solid tumors. Tjulandin S, Moiseyenko V, Semiglazov V, Manikhas G, Learoyd M, Saunders A, Stuart M, Keilholz U, Invest New Drugs 2014 32 145 153 10.1007/s10637-013-9963-6 23589215
15. A Phase I, open-label, dose escalation study of afatinib, in a 3-week-on/1-week-off schedule in patients with advanced solid tumors. Marshall J, Hwang J, Eskens FA, Burger H, Malik S, Uttenreuther-Fischer M, Stopfer P, Ould-Kaci M, Cohen RB, Lewis NL, Invest New Drugs 2013 31 399 408 10.1007/s10637-012-9890-y 23161335
16. A Phase I, open-label, dose-escalation study of continuous once-daily oral treatment with afatinib in patients with advanced solid tumors. Gordon MS, Mendelson DS, Gross M, Uttenreuther-Fischer M, Ould-Kaci M, Zhao Y, Stopfer P, Agus DB, Invest New Drugs 2013 31 409 416 10.1007/s10637-012-9904-9 23242861
17. Phase I and pharmacokinetic study of dacomitinib (PF-00299804), an oral irreversible, small molecule inhibitor of human epidermal growth factor receptor-1, -2, and -4 tyrosine kinases, in Japanese patients with advanced solid tumors. Takahashi T, Boku N, Murakami H, Naito T, Tsuya A, Nakamura Y, Ono A, Machida N, Yamazaki K, Watanabe J, Ruiz-Garcia A, Imai K, Ohki E, Yamamoto N, Invest New Drugs 2012 30 2352 2363 10.1007/s10637-011-9789-z 22249430
18. A phase I study with neratinib (HKI-272), an irreversible pan ErbB receptor tyrosine kinase inhibitor, in patients with solid tumors. Wong KK, Fracasso PM, Bukowski RM, Lynch TJ, Munster PN, Shapiro GI, Janne PA, Eder JP, Naughton MJ, Ellis MJ, Jones SF, Mekhail T, Zacharchuk C, Vermette J, Abbas R, Quinn S, Powell C, Burris HA, Clin Cancer Res 2009 15 2552 2558 10.1158/1078-0432.CCR-08-1978 19318484
19. Safety, efficacy and pharmacokinetics of neratinib (HKI-272) in Japanese patients with advanced solid tumors: a Phase 1 dose-escalation study. Ito Y, Suenaga M, Hatake K, Takahashi S, Yokoyama M, Onozawa Y, Yamazaki K, Hironaka S, Hashigami K, Hasegawa H, Takenaka N, Boku N, Jpn J Clin Oncol 2012 42 278 286 10.1093/jjco/hys012 22371427
20. Guiding principles for the clinical pharmacokinetics of chemical drugs http://www.sda.gov.cn/WS01/CL1616/83420.html
21. 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. Burris HR, Hurwitz HI, Dees EC, Dowlati A, Blackwell KL, O'Neil B, Marcom PK, Ellis MJ, Overmoyer B, Jones SF, Harris JL, Smith DA, Koch KM, Stead A, Mangum S, Spector NL, J Clin Oncol 2005 23 5305 5313 10.1200/JCO.2005.16.584 15955900
22. Pharmacokinetics and pharmacodynamics: maximizing the clinical potential of Erlotinib (Tarceva). Hidalgo M, Bloedow D, Semin Oncol 2003 30 25 33
23. Single-dose clinical pharmacokinetic studies of gefitinib. Swaisland HC, Smith RP, Laight A, Kerr DJ, Ranson M, Wilder-Smith CH, Duvauchelle T, Clin Pharmacokinet 2005 44 1165 1177 10.2165/00003088-200544110-00004 16231967
24. Phase I trial of the irreversible EGFR and HER2 kinase inhibitor BIBW 2992 in patients with advanced solid tumors. Yap TA, Vidal L, Adam J, Stephens P, Spicer J, Shaw H, Ang J, Temple G, Bell S, Shahidi M, Uttenreuther-Fischer M, Stopfer P, Futreal A, Calvert H, de Bono JS, Plummer R, J Clin Oncol 2010 28 3965 3972 10.1200/JCO.2009.26.7278 20679611
25. Detection of mutations in EGFR in circulating lung-cancer cells. Maheswaran S, Sequist LV, Nagrath S, Ulkus L, Brannigan B, Collura CV, Inserra E, Diederichs S, Iafrate AJ, Bell DW, Digumarthy S, Muzikansky A, Irimia D, Settleman J, Tompkins RG, Lynch TJ, Toner M, Haber DA, N Engl J Med 2008 359 366 377 10.1056/NEJMoa0800668 18596266
26. Southwest Oncology Group study S0413: a phase II trial of lapatinib (GW572016) as first-line therapy in patients with advanced or metastatic gastric cancer. Iqbal S, Goldman B, Fenoglio-Preiser CM, Lenz HJ, Zhang W, Danenberg KD, Shibata SI, Blanke CD, Ann Oncol 2011 22 2610 2615 10.1093/annonc/mdr021 21415234
27. Lapatinib in combination with capecitabine plus oxaliplatin (CapeOx) in HER2-positive advanced or metastatic gastric, esophageal, or gastroesophageal adenocarcinoma (AC): The TRIO-013/LOGiC Trial. Hecht JR, Bang YJ, Qin SQ, Chuang HC, Xu JM, Park JO, Jeziorski K, Shparyk Y, Hoff PM, Sobrero AF, Salman P, Li J, J Clin Oncol 2013 31 4001
28. A randomized, open-label, phase III study of lapatinib in combination with weekly paclitaxel versus weekly paclitaxel alone in the second-line treatment of HER2 amplified advanced gastric cancer (AGC) in Asian population: Tytan study. Bang YJ, J Clin Oncol 2012 30 11 10.1200/JCO.2011.35.4639 22105826