Leflunomide manufacturers and suppliers

Leflunomide suppliers

Properties

Melting point:: 166.5 °C

Boiling point:: 289.3±40.0 °C(Predicted)

Density: 1.392±0.06 g/cm3(Predicted)

storage temp.: 2-8°C

solubility: Practically insoluble in water, freely soluble in methanol, sparingly soluble in methylene chloride.

pka: 10.8(at 25℃)

color: White

Merck: 14,5432

Stability:: Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 1 month.

InChIKey: VHOGYURTWQBHIL-UHFFFAOYSA-N

Safety Information

Symbol(GHS): GHS06

Signal word: Danger

Hazard statements: H301-H315-H319-H335

Precautionary statements: P261-P264-P270-P301+P310-P302+P352-P305+P351+P338

Hazard Codes: Xn,Xi

Risk Statements: 22-36/37/38

Safety Statements: 26-36

RIDADR: UN 2811 6.1/PG 3

WGK Germany: 3

RTECS: NY2354200

HazardClass: 6.1

PackingGroup: III

HS Code: 2934990002

Use

Leflunomide (Arava), an isoxazole prodrug, is an orally activeDMARD marketed in 1998 for the treatment of RA. Itis well absorbed and extensively metabolized in vivo to itsactive metabolite, 2-cyano-3-hydroxy-2-buteneamide (teriflunomide),resulting from a reductive ring opening of theisoxazole ring. Unlike MTX, teriflunomideblocks T-cell proliferation by inhibiting dihydroorotate dehydrogenase,the rate-limiting enzyme in the de novobiosynthesis of pyrimidine that is believed to be responsiblefor the immunosuppressive properties of leflunomide.For this reason, it is not surprising that leflunomide has avery comparable therapeutic efficacy to the first-lineDMARD, MTX as shown in several extended open clinicaltrials. However, even though leflunomide is well toleratedlike MTX, several cases of toxic neuropathy have beenobserved during its use, thus careful monitoring of the patient’sneurological status during treatment is mandatory.Like MTX, leflunomide is contraindicated in pregnancy orin women considering pregnancy.

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