Drug intelligence / Profile preview

MLN2480 + MLN0128

Development stage
Phase 1
Lead developer
Takeda
Modality
Small Molecules
Administration
Oral
01

Overview

**MLN2480 + MLN0128** is an investigational, oral combination therapy used in clinical trials for advanced nonhematologic malignancies (solid tumors). - **MLN2480** (also known as TAK-580, DAY101) is a pan-RAF kinase inhibitor targeting A-RAF, B-RAF, and C-RAF, which are kinases downstream of RAS in the MAPK signaling pathway. By inhibiting these, MLN2480 interferes with tumor cell proliferation and survival that are dependent on MAPK pathway activation. - **MLN0128** (also known as TAK-228) is a dual mTORC1 and mTORC2 inhibitor, designed to block both complexes of the mammalian target of rapamycin (mTOR), a key regulator of cell growth, proliferation, metabolism, and survival. This dual inhibition may overcome resistance seen with drugs that only inhibit mTORC1. The combination aims to simultaneously inhibit signaling through the RAF/MEK/ERK and PI3K/AKT/mTOR pathways, which are frequently dysregulated in cancer and may act synergistically to inhibit tumor growth[1][4][7][10]. Both agents are administered orally.

02

Targets

RAF1 (c-Raf-1 (Y340D/Y341D))Mechanistic target of rapamycin complex 1Mechanistic target of rapamycin kinase complex 2

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