| Name | Iptacopan |
| Description | Iptacopan (LNP023) is an inhibitor with high affinity to factor B, with a KD value of 7.9 nM and an IC50 value of 10 nM. |
| In vitro | METHODS: Blood from three patients was analyzed in 2-14 replicates and Iptacopan was used at 1 μM. Hemolysis of PNH erythrocytes was determined by FACS analysis.
RESULTS LNP023 can block C3 deposition on the surface of CD59-negative red blood cells. [2] |
| In vivo | METHODS: Iptacopan (LNP023) was tested in KRN-induced arthritis at doses of 20, 60 and 180 mg/kg by injection twice daily.
RESULTS Comprehensive disease protection was observed at 60 and 180 mg/kg, and LNP023 significantly inhibited complement activation in joints at all doses, with significant reductions in Ba, C3d, and C5a levels. [1]
METHODS: Sixty-eight patients with biopsy-proven C3G, decreased C3 (<77 mg/dl), proteinuria ≥1.0 g/g), and estimated glomerular filtration rate (eGFR) ≥30 ml/min per 1.73 m2 were recruited. Patients will be randomized 1:1 to receive iptacopan 200 mg twice daily or placebo for 6 months, followed by open-label treatment of all patients with iptacopan 200 mg twice daily for 6 months.
RESULTS Iptacopan slows disease progression by inhibiting FB and preventing excessive activation of AP and may become one of the first targeted therapies available for C3G patients. [3] |
| Storage | 02 | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 5 mg/mL (11.83 mM), Sonication is recommended.
DMSO : 255 mg/mL (603.52 mM), Sonication is recommended.
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| Keywords | LNP-023 | LNP 023 | Iptacopan |
| Inhibitors Related | EG01377 2HCl | Iptacopan hydrochloride | BCX 1470 hydrochloride | Complement C5-IN-1 | Avacopan | ADH-503 | CP-289 | Dexamethasone acetate | Dexamethasone | Cyclosporin A | Dextran sulfate sodium salt (MW 5000) | 3-Phenoxybenzaldehyde |
| Related Compound Libraries | FDA-Approved & Pharmacopeia Drug Library | Bioactive Compound Library | Approved Drug Library | ReFRAME Related Library | Toxic Compound Library | Drug Repurposing Compound Library | Inhibitor Library | FDA-Approved Drug Library | Orally Active Compound Library | Immunology/Inflammation Compound Library | Clinical Compound Library | Bioactive Compounds Library Max |
United States
