巴瑞克替尼(Baricitinib)治疗脱发的原理,用法,疗效及副作用？

About Baricitinib

Developed jointly by Eli Lilly and Company and Incyte, it is a once-daily oral JAK inhibitor mainly used for the treatment of inflammatory and autoimmune diseases.

巴瑞克替尼(Baricitinib)可逆抑制Janus激酶1，其半最大抑制浓度(IC50)为5.9nM，而Janus激酶2的最大抑制浓度(IC50)为5.7 nM。 Through the signal transduction pathway of STAT proteins, gene expression in immune cells is ultimately regulated.

In December 2016, the European Committee for Medicinal Products for Human Use (CHMP) recommended the approval of baricitinib as a treatment for RA. In April 2018, Eli Lilly and Company and Incyte announced the approval of 2 mg baricitinib as a once-daily oral medication for the treatment of adult patients with moderately to severely active rheumatoid arthritis (RA) who have an inadequate response to or are intolerant to methotrexate.

Efficacy and role

Baricitinib is a Janus kinase (JAK) inhibitor. JAK is a type of intracellular enzyme that transmits signals generated by cytokine or growth factor-receptor interactions on the cell membrane and affects cellular processes of hematopoietic and immune cell function.

In the signaling pathway, JAKs phosphorylate and activate signal transducers and activators of transcription (STATs) that regulate intracellular activity, including gene expression. Baricitinib regulates signaling pathways at JAKs points and prevents STATs phosphorylation and activation.

In a cell-free separase assay, baricitinib had greater inhibitory potency at JAK1, JAK2, and TYK2 compared with JAK3. In human leukocytes, baricitinib inhibits cytokine-induced STAT phosphorylation mediated by JAK1/JAK3, JAK1/JAK2, JAK1/TYK2, or JAK2/TYK2 with equivalent effect.

How Baricitinib treats hair loss

Alopecia areata (AA) is a relapsing, chronic, immune-mediated disease characterized by non-persistent inflammatory hair loss that can affect any site of hair growth. The clinical manifestations of AA vary. Its pathogenesis involves immune and genetic factors as well as several pro-inflammatory cytokines involved in the pathogenesis of AA, including interleukin-15 and interferon-γ, as well as Th2 cytokines such as IL-4/IL-13 that signal through the Janus kinase (JAK) pathway.

The purpose of AA treatment is to stop its progression and reverse hair loss, and JAK inhibition has been shown to stop hair loss and reverse hair loss and has shown promising results in treating AA in clinical trials.

巴瑞克替尼(Baricitinib)是一种口服、可逆、选择性JAK1/JAK2抑制剂，在一项2期试验和最近的两项3期试验(BRAVE-AA1和BRAVE-AA2)中，对患有严重AA的成年人进行36周治疗后，其毛发生长表现优于安慰剂。

How to use Baricitinib to treat hair loss

Baricitinib is recommended to be taken with or without food. If the effect is not good, the dose can be increased to 4mg daily.

For patients with almost all or all hair loss, regardless of whether there is substantial loss of eyelashes or eyebrows, a dose of 4 mg once a day can be considered. Once the patient has adequately responded to 4 mg of medication once daily, reduce the dose to 2 mg once daily.

Side effects of Baricitinib in treating hair loss

In one study, the most common adverse events associated with baricitinib in alopecia areata were upper respiratory tract infection, urinary tract infection, acne, headache, and increased creatine kinase levels.

Side effects treatment methods

1. Upper respiratory tract infection: It is recommended that patients drink more water. Patients can receive symptomatic treatment under the guidance of a doctor. For example, patients with fever can use antipyretic drugs, and patients with cough can use antitussive drugs.

2. Urinary tract infection: Patients can be treated with antibiotics such as amoxicillin, drink more water, and urinate frequently.

3. Acne: It is recommended that patients pay attention to facial cleanliness and avoid using irritating toiletries. They can use erythromycin ointment, adapalene gel and other drugs to relieve symptoms.

4. Other side effects: If the patient also experiences other serious adverse reactions, he or she can seek medical treatment in time, consult a doctor, and deal with it under the guidance of a doctor.

Efficacy of Baricitinib in the treatment of hair loss

Background: The Food and Drug Administration has not approved a treatment for alopecia areata.

Purpose: In the phase 2 study of adult alopecia areata (BRAVE-AA1), evaluate the efficacy and safety of baricitinib in patients with scalp hair loss ≥50%.

Methods: Patients were randomized in a 1:1:1:1 ratio to receive placebo or once-daily doses of 1 mg, 2 mg, or 4 mg of baricitinib. Two consecutive interim analyzes were performed after all patients completed weeks 12 and 36 or discontinued treatment before these time points. The primary endpoint was the proportion of patients with a Severity Alopecia Tool (SALT) score ≤20 at week 36. For missing data, logistic regression was used to impute non-responders.

Results: A total of 110 patients were randomized (placebo group, 28; baricitinib 1-mg, 28; 2-mg, 27; 4-mg, 27). The baricitinib 1-mg dose was withdrawn after the first interim analysis based on lower SALT30 response rates. At Week 36, a significantly higher proportion of patients in the baricitinib 2-mg group (33.3%, P = .016) and 4-mg group (51.9%, P = .001) had a salt score ≤20 compared with the placebo group (3.6%). Baricitinib was well tolerated and there were no new safety findings.

Conclusion: These results support the safety and efficacy of baricitinib in ≥50% of patients with scalp disease.

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