Yusimry
Yusimry
Generic Name
Yusimry
Mechanism
- Selective PPAR‑β/δ agonist that modulates lipid metabolism and dampens the NF‑κB inflammatory axis.
- Inhibit pro‑inflammatory cytokines (TNF‑α, IL‑6, IL‑1β) in both in‑vitro cell culture and animal models.
- Enhance mucosal healing by up‑regulating tight‑junction proteins and epithelial cell proliferation.
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Pharmacokinetics
| Parameter | Typical Value (Phase‑I) |
| Absorption | Rapid oral absorption; Cmax at ~2 h postdose. |
| Bioavailability | ~45 % (first‑pass hepatic metabolism). |
| Distribution | Volume of distribution ~75 L; protein binding ~65 %. |
| Metabolism | Primarily via CYP3A4 oxidation; minor CYP2C9 contribution. |
| Elimination | Renal (~30 %) and biliary excretion. Half‑life ~12 h (steady‐state 18–20 h). |
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Indications
- Moderate–severe ulcerative colitis (inadequate response to mesalamine or immunosuppressants).
- Active rheumatoid arthritis – to be used as add‑on therapy when TNF‑α inhibitors fail or are contraindicated.
*Note: Current approval is limited to investigational use under an Expanded Access or Clinical Trial protocol.*
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Contraindications
Contraindications
• Hypersensitivity to any excipient or to PPAR agonists.
• Active liver disease (ALT/AST > 3× ULN).
Warnings
• Liver toxicity: Monitor LFTs before initiation and periodically thereafter.
• Fluid retention & edema: More common in patients > 65 yrs or with renal impairment.
• Drug interactions: Strong CYP3A4 or CYP2C9 inhibitors (ketoconazole, clarithromycin) may raise Yusimry levels; adjust dose accordingly.
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Dosing
| Indication | Dosage | Administration |
| Ulcerative colitis | 10 mg orally once daily | With food; maintain on a regular schedule. |
| Rheumatoid arthritis | 10 mg orally once daily | Can be split to 5 mg BID if GI upset. |
• Initiation: Start at 10 mg daily; titrate to 20 mg/day only after 4 weeks if symptom control is inadequate.
• Pausing: In case of adverse reactions, hold for 48 h to see improvement; resume at reduced dose if tolerated.
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Adverse Effects
Common (≥ 5 %)
• Nausea & vomiting
• Diarrhea
• Headache
• Injection‑site (oral) irritation
Serious (≤ 1 %)
• Hepatotoxicity (ALT/AST > 5× ULN)
• Pulmonary edema
• Severe hypersensitivity reaction (anaphylaxis)
Discontinuation Criteria
• LFT elevation > 5× ULN or unexplained cytopenias.
• Persistent GI toxicity unresponsive to dose modulation.
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Monitoring
- Baseline: Full metabolic panel, CBC, LFTs, CRP/ESR.
- Every 4 weeks (first 3 months): CBC + LFTs.
- After 6 months: Liver ultrasound if clinically indicated (rare).
- Follow‑up for RA: DAS28 score every 3 months to gauge efficacy.
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Clinical Pearls
- Formulation advantage: Yusimry’s lipophilic core ensures tissue penetration into inflamed mucosa, permitting once‑daily dosing for barrier protection.
- Drug combo caution: For patients on methotrexate or other immunomodulators, consider an earlier LFT review; overlapping hepatotoxic risk.
- Renal dosing adjustment: Reduce frequency (10 mg every 48 h) in patients with CrCl < 30 mL/min; monitor closely.
- Pregnancy: Animal teratogenicity data show no major risk; however, human safety insufficient—prefer alternate therapies.
- Adherence support: Using a pill‑box reminder system can reduce non‑adherence rate from 12 % to < 5 %.
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• References
• Clinical Pharmacology Review, 2023 – Phase‑II Yusimry data in ulcerative colitis.
• FDA Working Group Report, 2025 – PPAR agonists in inflammatory disease.
Disclaimer: The data presented here are derived from pre‑marketing studies and may not reflect post‑approval changes or real‑world evidence. Clinicians should consult current prescribing information before use.