A pilot, pharmacokinetic (PK), and pharmacodynamic (PD) study to determine the feasibility of intrapatient dose escalation to tolerable rash and the activity of maximal doses of erlotinib (E) in previously treated patients with advanced non-small cell lung cancer (NSCLC)

Mita, C.; Schwartz, Gary N.; Mita, Monica; Papadopoulos, K.; Wood, Laura S.; Jonge, M. de; Yancik, S.; Hamilton, Marta; Santabárbara, P.; Rowinsky, Eric K.

doi:10.1200/jco.2005.23.16_suppl.3045

Cited by 7 publications

(3 citation statements)

References 0 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…For example, a recent study of NSCLC patients receiving erlotinib first line in combination with docetaxel defined the MTD as 200 mg/d 18 . Furthermore, a study is ongoing to investigate if the dose of erlotinib can be escalated above the current MTD in individual patients using the onset of rash as the stopping rule 19 …”

mentioning

confidence: 99%

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

Frohna¹,

Lu²,

Eppler³

et al. 2006

The Journal of Clinical Pharma

View full text Add to dashboard Cite

A randomized, open-label, 2-period crossover study was conducted to evaluate the bioequivalence of 6 tablets of erlotinib 25 mg and 1 tablet of erlotinib 150 mg (arm A, n = 42) and the oral bioavailability of the 150-mg tablet versus a 25-mg intravenous infusion (arm B, n = 20) in healthy subjects. The washout period was 2 weeks between treatments. Plasma concentrations of erlotinib and its active metabolite, OSI-420, were measured after each dose. The ratios of geometric means for AUC(0-infinity) and Cmax of erlotinib following 6 tablets of erlotinib 25 mg and 1 tablet of erlotinib 150 mg were (1 and 0.95) within the predefined bioequivalence range of 0.80 to 1.25. The mean absolute oral bioavailability, using compartmental analysis, was estimated as 59% (95% confidence interval, 55%-63%). Overall, 6 tablets of erlotinib 25 mg are bioequivalent to a single 150-mg tablet. Both intravenous and oral erlotinib were generally well tolerated with an estimated bioavailability of 59% following oral administration.

show abstract

mentioning

confidence: 99%

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

Frohna¹,

Lu²,

Eppler³

et al. 2006

The Journal of Clinical Pharma

View full text Add to dashboard Cite

show abstract

“…However, titration of erlotinib to skin rash in an attempt to optimize efficacy is likely to be difficult given that diarrhea has been demonstrated as the main dose-limiting toxicity. A dose-to-rash study is currently ongoing with erlotinib in lung cancer to explore this issue further ( Mita et al 2005 ).…”

Section: Selection Of Patients For Therapymentioning

confidence: 99%

Role of erlotinib in the management of pancreatic cancer

Starling¹,

Neoptolemos²,

Cunningham³

2006

Therapeutics and Clinical Risk Management

View full text Add to dashboard Cite

Pancreatic cancer is a largely chemo-resistant disease with a poor prognosis. Despite the adoption of gemcitabine monotherapy as a standard of care, outcomes remain poor. Until recently randomized phase III studies have not demonstrated superiority of various cytotoxic combinations or a number of the newer biologic targeted drugs. The situation has changed with capecitabine and erlotinib, either of which in combination with gemcitabine produces a small increase in survival. Erlotinib is a small molecule tyrosine kinase inhibitor against epidermal growth factor receptor which has an important role in the molecular pathogenesis of pancreatic cancer. In both pre-clinical and early clinical evaluation it has shown anti-tumor activity against pancreatic cancer in combination with gemcitabine. A randomized phase III study in locally advanced and metastatic pancreatic cancer has shown a survival advantage for the combination of gemcitabine plus erlotinib over gemcitabine alone. The rationale for the clinical development of erlotinib in combination with gemcitabine in pancreatic cancer culminating in this randomized trial, together with pharmacologic, toxicity and patient selection considerations form the focus of this review.

show abstract

“…The MTD needs to be further defined in smokers, as this population of patients may require a higher erlotinib dose than that currently used to achieve the same level of drug exposure in nonsmokers. Preliminary results of a study of the feasibility of dose escalation with erlotinib in patients with NSCLC were presented at this year's Annual Meeting of the American Society of Clinical Oncology [10].…”

Section: Mtd Is Important and Dose Escalation May Be Appropriate In Smentioning

confidence: 99%

The Current Situation: Erlotinib (Tarceva®) and Gefitinib (Iressa®) in Non-Small Cell Lung Cancer

Comis

2005

The Oncologist

View full text Add to dashboard Cite

A pilot, pharmacokinetic (PK), and pharmacodynamic (PD) study to determine the feasibility of intrapatient dose escalation to tolerable rash and the activity of maximal doses of erlotinib (E) in previously treated patients with advanced non-small cell lung cancer (NSCLC)

Cited by 7 publications

References 0 publications

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

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

Role of erlotinib in the management of pancreatic cancer

The Current Situation: Erlotinib (Tarceva®) and Gefitinib (Iressa®) in Non-Small Cell Lung Cancer

Contact Info

Product

Resources

About