Selumetinib (Koselugo (approved for neurofibromatosis), AZD6244, ARRY-142886)
Targeted Therapy
Description
Selumetinib is an oral MEK1/2 inhibitor that has been evaluated in colorectal cancer patients, particularly those with KRAS, BRAF, and EGFR mutations. This targeted therapy blocks the MEK protein in the RAS/RAF/MEK/ERK signaling pathway, which is frequently dysregulated in colorectal malignancies. Selumetinib has been tested both as monotherapy and in combination with chemotherapy agents like irinotecan in patients with advanced colorectal carcinoma who have received prior treatment.
Mechanism of Action
Selumetinib selectively inhibits mitogen-activated protein kinase kinase 1 and 2 (MEK1/2), which are critical components of the RAS/RAF/MEK/ERK pathway. By blocking MEK1/2, selumetinib prevents the phosphorylation and activation of ERK1/2, thereby disrupting downstream signaling that promotes tumor cell proliferation and survival. This mechanism is particularly relevant in colorectal cancers with RAS or RAF mutations where this pathway is constitutively activated.
Molecular Targets
Side Effects
Not all side effects are listed. Side effects vary by individual. Always consult your oncologist.
Clinical Trials
Quick Info
| Brand Name | Koselugo (approved for neurofibromatosis), AZD6244, ARRY-142886 |
| Category | Targeted Therapy |
 Status | Experimental |
 EMA Status | EMA Approved |
 Spain Access | Hospital use off-label in CRC |
| Administration | Oral |
| Clinical Trials | 9 |
Related Medications
Medical Disclaimer
This information is for educational purposes only and should not replace professional medical advice. Always consult your healthcare team before making treatment decisions.