Description

Leflunomide Tablets

Leflunomide Tablets USP / BP / IP (10 mg / 20 mg / 100 mg)

High-Potency Isoxazole Disease-Modifying Anti-Rheumatic Drug (DMARD)

Healthy Life Pharma Private Limited, alongside our specialized global export and marketing division Healthy Inc, is an authorized manufacturer, CDMO services provider, and wholesale exporter of advanced rheumatology, immunology, and musculoskeletal therapeutics. We manufacture ultra-high-purity, chemically stable Leflunomide Tablets within our state-of-the-art, WHO–GMP certified, high-containment solid dosage manufacturing facilities.

Serving as a primary frontline therapeutic milestone for arresting progressive joint destruction, this specialized immunomodulator represents a vital strategic export to rheumatology clinic networks, state healthcare procurement pipelines, public hospital emergency reserves, and international digital B2B pharmaceutical marketplaces across the CIS region, Sub-Saharan Africa, LATAM, and South-East Asia.

Product Overview

This formulation operates as an “Immune Cell Pyrimidine Depletion Catalyst.” It ensures systemic structural stabilization and prevents joint degradation by cutting off the specialized genetic building blocks required by hyperactive, auto-aggressive white blood cells to multiply, safely halting the autoimmune attack.

• Mechanism 1 (Active Metabolite Conversion): Leflunomide is an isoxazole derivative prodrug. Upon oral ingestion, it undergoes rapid and near-complete physical pre-systemic conversion during its first pass through the gut wall and liver into its active malononitrilamide metabolite, Teriflunomide ($A77\,1726$).

• Mechanism 2 (Dihydroorotate Dehydrogenase Blockade): The active metabolite $A77\,1726$ physically attaches to and competitively inhibits Dihydroorotate Dehydrogenase (DHODH), a critical mitochondrial enzyme.

• Mechanism 3 (Lymphocyte Clonal Arrest): DHODH is the rate-limiting enzyme in the de novo synthesis pathway of uridine monophosphate ($UMP$), an essential pyrimidine building block. While normal body cells can recycle pyrimidines, hyperactive auto-aggressive T- and B-lymphocytes rely entirely on de novo synthesis to replicate. By blocking this enzyme, Leflunomide starves these cells of pyrimidines, arresting them in the $G_{1}$ cellular phase to completely suppress the autoimmune attack on joint cartilage and synovial tissues.

Product Composition & Available Portfolio Strengths

We supply Leflunomide across the complete compendial strength matrix, enabling clinicians to manage both rapid initial loading cycles and long-term low-dose maintenance blocks.

Technical & Logistics Specifications

• HS Code: 3004.90.99 (Medicaments acting on the musculoskeletal system / Immunomodulators / DMARDs)

• CAS Number: 75706-12-6 (Leflunomide) / 163451-81-8 (Active Metabolite Teriflunomide)

• Dosage Form: Oral Solid Film-Coated Tablet (Core matrix precisely film-coated to shield the active isoxazole structure from light-induced degradation and moisture-induced cleavage)

• Packaging Configurations: 10 / 14 / 30 Tablets per Blister Strip packed exclusively in high-barrier Alu-Alu (Cold-Form Foil) matrix configurations. Leflunomide is highly sensitive to environmental moisture vapor; our tropicalized opaque configurations isolate the core, guaranteeing a full 36-month shelf life in hot, humid Zone IVb export environments.

Specialty Manufacturing Governance & Quality Control

• High-Containment Cleanroom Isolation: Because Leflunomide is a highly potent immunomodulator with low-dose active operations, our production runs occur within Dedicated, Air-Pressure Segregated Cleanroom Blocks. Fully independent, HEPA-filtered HVAC infrastructures physically isolate these lines to guarantee absolute zero active cross-contamination into non-immunological product streams.

• Precision Micro-Granulation Uniformity: Due to the low mass of active Leflunomide (10 mg to 20 mg) relative to the total tablet weight matrix, we deploy Automated High-Shear Wet Granulation Blending Suites, physically ensuring perfect chemical content uniformity down to the microgram across millions of compressed units.

• Validated Release Profiles: Every export production batch physically undergoes strict Automated In-Vitro Dissolution Profiling, chemically validating that our generic tablets achieve fast gastric disintegration and immediate absorption curves to match global innovator references (such as Arava).

Primary Indications

• Rheumatology: First-line disease-modifying treatment of active Rheumatoid Arthritis (RA) in adult populations to reduce signs/symptoms and retard structural joint damage.

• Dermatology & Rheumatology Support: Medical management of active Psoriatic Arthritis presenting with concurrent cutaneous lesions.

Usage Instructions

• Administration Matrix: Swallow the tablet physically whole with a glass of water. It can be taken consistently either with or without food.

• The Extended Half-Life Reality: The active metabolite $A77\,1726$ binds extensively to plasma albumin and exhibits an exceptionally long elimination half-life of 2 weeks. Because of this, therapeutic steady-state results physically take several weeks to manifest, and the drug remains in the system long after therapy stops.

• The Cholestyramine Washout Protocol: Advise clinical networks that due to its long half-life, if a patient requires rapid drug removal due to unexpected toxicity or pregnancy planning, a physical Cholestyramine Drug Elimination Washout Protocol must be initiated. Administering 8g of cholestyramine orally three times daily for 11 days drops active plasma levels below 0.02 mg/L.

• Strict Hepatic Enzyme Tracking: Leflunomide is heavily cleared via hepatic metabolic paths. It is clinically mandatory to perform baseline and regular periodic tracking of Alanine Aminotransferase ($ALT$) and Aspartate Aminotransferase ($AST$) transaminase levels throughout active therapy runs.

Safety Warning: POTENT IMMUNOMODULATOR & FIRST-LINE DMARD. For Rheumatology and Immunology Specialist Supervision Only. The Black Box Teratogenicity Mandate: ABSOLUTELY CONTRAINDICATED IN PREGNANCY & WOMEN OF CHILDBEARING POTENTIAL. Leflunomide chemically induces severe, life-threatening fetal malformations and death. Pregnancy must be strictly excluded before initialization. Women must maintain strict double-barrier contraception throughout treatment and must never attempt conception until a verified cholestyramine washout protocol has physically brought active plasma levels down below safety thresholds. Severe Hepatotoxicity Warning: May chemically induce severe transaminase elevations; discontinue therapy immediately if $ALT$ levels rise greater than three times the upper limit of normal. Contraindications: Absolute contraindications in pregnant or lactating patients, severe underlying hepatic impairment, severe immunodeficiency states, severe uncontrolled infections, or known hypersensitivity to isoxazole matrices.

Global CDMO Services & Specialty Tender Logistics

Healthy Life Pharma Private Limited and Healthy Inc provide complete, internationally validated Third-Party Contract Manufacturing (CDMO Services) and bulk private-label export pipelines for the entire Leflunomide dosage spectrum. Operating under strict specialty immunomodulator containment protocols, we prepare all mandatory cross-border documentation (WHO-GMP Certificate, Certificates of Pharmaceutical Product – COPP, Certificates of Analysis – COA, Zone IVb Stability Reports, and Complete CTD Format Dossier sets) for rapid entry registration and seamless import entry.

Commercial & Bulk Procurement Inquiries:

• Corporate Head Office: Mumbai, Maharashtra, India

• Primary Manufacturing Base: Boisar, Maharashtra, India

• WhatsApp / Direct Regulatory Helpline: +91 7710003340

• Specialty Registry Email: info@healthyinc.co.in