Ruxolitinib is a small molecule kinase inhibitor type pharmaceutical active ingredient that has found application in the treatment of certain hematological disorders. Some key areas where ruxolitinib API is utilized include:

Myelofibrosis

The main FDA approved application for ruxolitinib is in the treatment of myelofibrosis. Myelofibrosis is a rare bone marrow disorder that results in abnormal scar tissue formation, leading to enlarged spleen, anemia, and other complications. Ruxolitinib can reduce spleen size, improve quality of life, and help manage myelofibrosis symptoms.

Polycythemia Vera

Ruxolitinib is also approved for treatment of polycythemia vera, which involves overproduction of blood cells by bone marrow. It helps reduce blood cell count and manage associated symptoms like itching, enlarged spleen, and cardiovascular complications in polycythemia vera patients.

Graft vs Host Disease

There is interest in using ruxolitinib for steroid-refractory graft vs host disease, a complication of stem cell transplants. Ruxolitinib may regulate inflammatory cytokines involved in GVHD. It is currently being studied in clinical trials for this application.

Alopecia Areata

Topical ruxolitinib is under investigation for treatment of alopecia areata, an autoimmune condition causing hair loss. Early studies showed topical ruxolitinib improved hair regrowth. Ruxolitinib creams may help regrow hair by reducing localized inflammation.

Vitiligo

Vitiligo is a disorder causing skin depigmentation. It is believed to involve autoimmune targeting of melanocytes. Early clinical evidence suggests topical ruxolitinib may help repigment vitiligo spots by modulating the immune response in skin.

COVID-19 Cytokine Storm

Some severe cases COVID-19 infection are linked to dangerous levels of inflammatory cytokines dubbed “cytokine storm.” There is interest in using ruxolitinib's anti-inflammatory effects to potentially counteract severe inflammatory responses in COVID-19 patients.

Mechanism of Action

Ruxolitinib exerts its effects by inhibiting Janus Associated Kinases (JAKs), which are intracellular enzymes involved in cytokine signaling pathways that drive inflammatory responses. Specifically, ruxolitinib inhibits JAK1 and JAK2 over other JAK family enzymes.

By inhibiting JAK1/JAK2, ruxolitinib can modulate signaling of inflammatory cytokines like IL-6, interferons, and GM-SCF. This produces an overall anti-inflammatory effect that underlies ruxolitinib's therapeutic benefits.

Dosage Forms

Ruxolitinib API is utilized in the following pharmaceutical dosage forms:

• Tablets - 5mg, 10mg, 15mg, 20mg and 25mg for oral administration.
• Topical creams - Typically 1.5% or 2% creams for application to skin and scalp.

The tablets contain ruxolitinib phosphate, while the topical forms contain the free base. Ruxolitinib has also been studied for injection and suspension formulations.

Combination Therapies

Ruxolitinib is being studied in combination with other drugs for enhanced efficacy. Some examples include:

• With PEGINTRON® for myelofibrosis treatment
• With exon-skipping drugs for alopecia areata
• With ibrutinib for graft vs host disease

Combination strategies aim to leverage synergistic mechanisms and reduce drug resistance development.

Manufacturing Demand

As both oral and topical applications expand, global demand for high quality ruxolitinib API from pharmaceutical manufacturers continues to grow. Our advanced manufacturing capabilities and capacity helps ensure reliable supply of this critical active ingredient for current and emerging therapies.