CDK4/6 inhibitor LY2835219 Exhibits Early Evidence of Clinical Activity Against Solid Tumors

Share this content:

CHICAGO―The selective CDK4/6 inhibitor LY2835219 is safe in patients diagnosed with solid tumors, according to results of a first-in-human phase 1 dose-escalation clinical trial presented at the 2013 American Society of Clinical Oncology (ASCO) Annual Meeting.

“LY2835219 shows acceptable safety and early clinical activity as a single agent for patients with advanced cancer,” concluded lead author Geoffrey Shapiro, MD, PhD, of the Dana-Farber Cancer Institute in Boston, MA, and coauthors.

Early clinical activity has been observed in patients with ovarian cancer, non-small cell lung cancer (NSCLC), breast cancer, and melanoma, the coauthors reported.

LY2835219 has shown antitumor activity and “distributes efficiently to the brain” in preclinical mouse studies, the authors noted. The authors performed the phase 1 trial to evaluate this agent's safety and pharmacokinetics, and antitumor activity in 75 patients.

“3+3 dose escalation was followed by expansions in advanced cases of five tumor types (brain metastases permitted): NSCLC, glioblastoma, breast cancer, melanoma, and colorectal cancer,” they reported. “LY2835219 was taken orally every 12 or 24 hours (in escalation) and every 12 hours (in expansions) on days 1-28 of a 28-day cycle.”

The most frequent drug-related adverse events were diarrhea (52%; grade 3, 7%), nausea (30%; grade 3, 5%), fatigue (21%; grade 3, 5%), vomiting (21%; grade 3, 1%); and neutropenia (19%; grade 3, 7%), the coauthors reported.

“One patient with ovarian cancer had a durable CA-125 response with a greater than 50% decrease in 15 cycles,” the team reported. “One patient with KRAS mutant NSCLC had a 27% decrease by RECIST (Response Evaluation Criteria in Solid Tumors). One patient with CDKN2A -/- NRAS mutant melanoma had a confirmed partial response.”

Related Resources

You must be a registered member of Cancer Therapy Advisor to post a comment.

Sign Up for Free e-newsletters



Regimen and Drug Listings

GET FULL LISTINGS OF TREATMENT Regimens and Drug INFORMATION

Bone Cancer Regimens Drugs
Brain Cancer Regimens Drugs
Breast Cancer Regimens Drugs
Endocrine Cancer Regimens Drugs
Gastrointestinal Cancer Regimens Drugs
Gynecologic Cancer Regimens Drugs
Head and Neck Cancer Regimens Drugs
Hematologic Cancer Regimens Drugs
Lung Cancer Regimens Drugs
Other Cancers Regimens
Prostate Cancer Regimens Drugs
Rare Cancers Regimens
Renal Cell Carcinoma Regimens Drugs
Skin Cancer Regimens Drugs
Urologic Cancers Regimens Drugs