One of two molecules for this week
March 08, 2016
Rogaine, watch out for us!
What molecules are we?
Image of Tofacitinib and Ruxolitinib 3D Image of Tofacitinib and Ruxolitinib
Figure 1: Tofacitinib
Image of Tofacitinib and Ruxolitinib 3D Image of Tofacitinib and Ruxolitinib
Figure 2: Ruxolitinib

Tofacitinib (trade names Xeljanz and Jakvinus; Pfizer) and ruxolitinib (Jakafi and Jakavi; Incyte Pharmaceuticals and Novartis) are Janus kinase (JAK) inhibitors that are used to treat rheumatoid arthritis and myelofibrosis, respectively. Tofacitinib (structure 1) was the first to be developed; it was the outgrowth of research performed at the National Institutes of Health by John O'Shea and co-workers.

Ruxolitinib (structure 2) did not come along until about 5 years ago. It may also be useful for treating other disease such as lymphoma, pancreatic cancer, and polycythemia vera.

Both drugs are now being looked at to treat a very widespread but much less serious condition: hair loss. A Columbia University team led by Angela M. Christiano observed that administering the drugs orally to mice promoted hair growth. The downside was that the animals' immune systems were compromised, so the researchers applied the drugs topically and obtained similar hair growth results.

It turns out that JAK inhibition is the key to this effect as it is for disease treatment. The drugs inhibit a kinase pathway in dormant hair follicle cells that causes the cells to transcribe DNA. Inhibiting the pathway "wakes up" the cells, and hair growth ensues.

MOTW update: 
April 20, 2020

Ruxolitinib is a Janus kinase inhibitor originally used to treat myelofibrosis. In 2016, it was under investigation as a hair-loss preventive. It is now being considered to lessen the effects of COVID-19 by controlling extreme immune responses.

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