Drug intelligence / Profile preview

TD-1211 + itraconazole

Development stage
Unknown
Lead developer
Theravance Biopharma
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

TD-1211 + itraconazole is a combination of two drugs: - **TD-1211 (axelopran)** is a peripherally acting μ-opioid receptor antagonist developed by Theravance Biopharma and licensed to Glycyx. It also acts on κ-opioid and δ-opioid receptors with similar affinity for μ and κ receptors and lower affinity for δ. Its primary indication has been the treatment of opioid-induced constipation (OIC), aiming to alleviate gastrointestinal side effects of opioid therapy without affecting central analgesia. Axelopran does not significantly penetrate the CNS[1][2][3][4][6]. - **Itraconazole** is an antifungal agent that inhibits fungal cytochrome P450-dependent enzyme lanosterol 14α-demethylase, thereby impairing ergosterol synthesis in fungal cell membranes. There are no known marketed or clinical-stage products combining these two agents as a fixed-dose or co-packaged product; thus, this appears to be either an experimental or theoretical combination.

Other names
axelopran + itraconazoleTD-1211 + itraconazole
02

Targets

MOR (Mu opioid receptor)DOR (Opioid Receptor Delta 1)KOR (Kappa opioid receptor)

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