Some medications for atopic dermatitis


Regarding how to treat atopic dermatitis, I will introduce some related drugs without any medical advice. And because the specific symptoms of specific patients are different, the recommendations of regular medical institutions should prevail.

Introduction to Tacrolimus

Tacrolimus, also known as FK506, is a calcineurin inhibitor isolated from Streptomyces genus. It is a representative second-generation immunosuppressant drug. It mainly inhibits interleukin-2 (ⅠL- 2) Release and comprehensively inhibit the function of T lymphocytes. 100 times stronger than cyclosporine (CsA).

Tacrolimus capsules were developed by Astellas and were approved for marketing in Japan in 1993. Subsequently, the original tacrolimus capsules were approved in the United States in 1994 (trade name: PROGRAF) and in my country in 1998 (trade name: PROGRAF).

Tacrolimus is clinically mainly used to combat autoimmune diseases and rejection reactions after organ transplantation. As a first-line drug for liver and kidney transplantation, it has been marketed in 14 countries including Japan and the United States.

Clinical trials have shown that it has good efficacy in heart, lung, intestinal, bone marrow and other transplants. Adverse reactions are similar to those of cyclosporine.

At the same time, tacrolimus also plays an active role in the treatment of autoimmune diseases such as atopic dermatitis (AD), systemic lupus erythematosus (SLE), and autoimmune eye diseases.

There are many generic drugs of tacrolimus capsules and tacrolimus ointment on the market in China, and many of them have passed the consistency evaluation, confirming that the efficacy of the generic drugs is consistent with the original drug. The cost of medication is significantly reduced while ensuring the therapeutic effect.

Introduction to Pimecromus

Pimecrolimus is a derivative of the lipophilic and anti-inflammatory ascomycin macrolactam, which can inhibit the production and release of inflammatory cytokines and mediators by pre-T cells and macrophages, and is used for mild to moderate atopic dermatitis. (eczema) treatment.

The skin permeability of pimecrolimus cream is 70-110 times lower than that of glucocorticoids and 9-10 times lower than that of tacrolimus. It has lower systemic bioavailability and is safer. According to large-sample clinical research data, pimecrolimus cream has a rapid onset of effect in the treatment of infants and young children with atopic dermatitis. The 5-year efficacy is equivalent to that of infants and young children with atopic dermatitis who use glucocorticoids. It can effectively help patients with atopic dermatitis. Patients with atopic dermatitis should reduce the dosage of steroids. The safety profile for the treatment of mild to moderate infants and young children is good, and the risk of infection is equivalent to placebo.

On April 10, 2023, pimecrolimus cream was successfully approved in my country for the treatment of patients with mild to moderate atopic dermatitis 3 months and above, becoming the first and currently the only atopic dermatitis treatment in infants and young children in China. Non-hormonal topical medications.

Introduction to Criborole

Criborole (AN2728) is a nonsteroidal phosphodiesterase 4 (PDE-4) inhibitor. It was first developed by Anacor Pharmaceuticals. In May 2016, Pfizer acquired AnChemicalbookacor. In December of the same year, the US FDA approved criborole (AN2728) ointment (2% or 5%) for local treatment of minor symptoms in patients over 2 years old. Mild to moderate atopic dermatitis, brand name Eucrisa.

The biggest advantage of criborole is that it is a small-molecule, non-hormonal drug that can combine therapeutic effect and comfort, and even has almost no side effects for some patients. It is the first external dermatology drug to enter the clinical urgently needed new drug name Chemicalbook list. It can be said that the launch of Criborole has filled the treatment needs of atopic dermatitis in Chinese children and adults, breaking the status quo of no new products in the topical non-hormonal anti-inflammatory field for more than 10 years, and is of epoch-making significance.

Criborole is an inhibitor of phosphodiesterase 4 (PDE4). PDE4 is an enzyme involved in controlling the activity of inflammatory cells. PDE4 participates in IL-4/5 in inflammatory cells by controlling the degradation of cyclic adenosine monophosphate. The production of inflammatory factors such as /10/13 and prostaglandin PGE2 plays a role in improving the body's inflammatory response by inhibiting PDE4 activity. Clinical studies have shown that in patients aged 2 to 79 years with mild to moderate atopic dermatitis, treatment with criborole for 28 days resulted in significant relief and complete or near-complete resolution of the rash compared with placebo.

In December 2016, criborole was approved by the US FDA for marketing, becoming the first new molecular entity approved by the US FDA for the treatment of atopic dermatitis (AD) in the past 15 years. In July 2020, Chemicalbook Borro Ointment was approved for marketing in China, becoming China's first and only hormone-free PDE-4 inhibitor suitable for the treatment of mild to moderate atopic dermatitis in children and adult patients aged 2 years and above. Prescription topical medications.

Introduction to ruxolitinib cream

Ruxolitinib can competitively bind to ATP at the enzyme catalytic site and down-regulate abnormally activated signaling pathways to achieve therapeutic purposes. The JAK protein kinase family plays an important role in mediating the signaling of inflammatory cytokines and can quickly control itching and eliminate the inflammatory response faster than traditional biological agents.

In September 2021, the U.S. Food and Drug Administration (FDA) approved ruxolitinib cream (Opzelura) as a topical JAK inhibitor for non-immune patients 12 years and older whose condition is not advisable or cannot be adequately controlled by traditional topical prescription therapies. Short-term and non-sustaining chronic treatment of functionally impaired patients with mild to moderate atopic dermatitis (AD). In July 2022, the FDA approved the drug for the local treatment of non-segmental vitiligo in patients 12 years old and above. Currently, ruxolitinib cream is the first and only topical JAK inhibitor approved by the U.S. Food and Drug Administration (FDA).

On December 2, 2022, China Medical System, a listed company on the Hong Kong stock market, issued an announcement that through its subsidiary China Medical System and Nasnak’s boss biopharmaceutical company Incyte, the topical preparation of ruxolitinib (Ruxolitinib) is used to treat autoimmune inflammatory skin diseases. Cotinib Cream) entered into a cooperation and licensing agreement to obtain exclusive licensing rights for this product.

Special explanation

Ruxolitinib cream and ruxolitinib phosphate tablets have the same main ingredients, but have different trade names and different indications.

Ruxolitinib is a JAK1/2 inhibitor, and the original research company is Incyte. In 2009, Novartis reached a cooperation agreement with Incyte and obtained the commercialization rights of ruxolitinib in markets outside the United States.

Novartis is responsible for commercializing the tablets outside the United States under the trade name Jakavi.

Incyte is responsible for the development and commercialization of ruxolitinib in the United States under the trade name Jakafi.

Ruxolitinib phosphate tablets were first approved for marketing in the United States in November 2011.

The original ruxolitinib phosphate tablets (trade name: Jiekewei) were approved for marketing by the State Food and Drug Administration in China through the priority review process in March 2017.

Ruxolitinib phosphate tablets are indicated for the treatment of intermediate-risk or high-risk primary myelofibrosis (PMF), myelofibrosis secondary to polycythemia vera (PPV-MF), or bone marrow fibrosis induced by essential thrombocythemia. (PET-MF) in adult patients to treat disease-related splenomegaly or disease-related symptoms.