GDC-0276

A detailed overview of the investigational drug GDC-0276

GDC-0276 is an investigational drug that is being studied for its potential use in the treatment of various cancers. It is a small molecule inhibitor that targets specific pathways involved in cancer cell proliferation and survival.

Mechanism of Action

GDC-0276 functions primarily as a kinase inhibitor. It targets the PI3K/AKT/mTOR pathway, which is a critical signaling pathway that regulates cell growth, proliferation, and survival. By inhibiting this pathway, GDC-0276 aims to reduce the growth and spread of cancer cells.

Pharmacokinetics

The pharmacokinetic profile of GDC-0276 includes its absorption, distribution, metabolism, and excretion (ADME) characteristics. Studies have shown that GDC-0276 is orally bioavailable, with a half-life that supports once-daily dosing. It is metabolized primarily in the liver and excreted through both renal and fecal pathways.

Clinical Trials

GDC-0276 is currently undergoing clinical trials to evaluate its efficacy and safety in patients with various types of cancer, including breast cancer, lung cancer, and colorectal cancer. Early-phase trials have demonstrated promising results, with manageable side effects and evidence of anti-tumor activity.

Side Effects

Common side effects observed in clinical trials of GDC-0276 include nausea, fatigue, diarrhea, and rash. More serious adverse effects may include liver enzyme elevations and hematological abnormalities, which require careful monitoring during treatment.

Research and Development

GDC-0276 was developed by Genentech, a member of the Roche Group, as part of their oncology pipeline. The development of GDC-0276 is part of a broader effort to create targeted therapies that can improve outcomes for cancer patients by specifically inhibiting pathways that are dysregulated in cancer cells.

Also see

• PI3K inhibitors
• Targeted cancer therapy
• Clinical trials
• Oncology

Receptor Tyrosine Kinase Inhibitors

Name	Target	Indications	Notes
Imatinib	BCR-ABL	Chronic myeloid leukemia, Gastrointestinal stromal tumor	First approved RTK inhibitor
Erlotinib	EGFR	Non-small cell lung cancer, Pancreatic cancer	Used in combination with gemcitabine for pancreatic cancer
Sunitinib	VEGFR, PDGFR	Renal cell carcinoma, Gastrointestinal stromal tumor	Multi-targeted RTK inhibitor
Gefitinib	EGFR	Non-small cell lung cancer	First EGFR inhibitor approved
Sorafenib	VEGFR, RAF kinase	Hepatocellular carcinoma, Renal cell carcinoma	Also inhibits RAF kinases
Lapatinib	HER2/neu, EGFR	Breast cancer	Used in combination with capecitabine