Drug intelligence / Profile preview

mipomersen + warfarin

Development stage
Phase 1
Lead developer
Sanofi
Modality
Antisense Oligonucleotides (ASOs) → Long RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics, Single-strand DNA → Antisense DNA → DNA Therapeutics → Nucleic Acid Therapeutics, Modified DNA Oligonucleotides → Antisense DNA → DNA Therapeutics → Nucleic Acid Therapeutics, Small Molecules
Administration
Subcutaneous, Oral
01

Overview

mipomersen + warfarin is a combination of two pharmaceutical agents: mipomersen, a second-generation antisense oligonucleotide, and warfarin, a vitamin K antagonist anticoagulant. Mipomersen is indicated as an adjunct therapy for lowering low-density lipoprotein cholesterol (LDL-C), apolipoprotein B (apoB), total cholesterol, and non-high-density lipoprotein cholesterol in adults with homozygous familial hypercholesterolemia (HoFH)[1][2][3][4]. Its mechanism of action involves hybridizing to apoB-100 mRNA, leading to RNase H-mediated degradation and inhibition of apoB protein synthesis[4]. Warfarin inhibits vitamin K epoxide reductase, thereby reducing functional vitamin K and suppressing synthesis of vitamin K-dependent clotting factors II, VII, IX, and X. A clinically studied drug-drug interaction demonstrated that concurrent administration of mipomersen and warfarin does not result in clinically relevant pharmacokinetic or pharmacodynamic interactions, or increased bleeding risk[1][3][4][5].

Other names
mipomersen sodiumwarfarin sodium
02

Targets

VKORC1 (Vitamin K epoxide reductase complex subunit 1)ApoB-100 (Apolipoprotein B-100)

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