伊曲莫德(Etrasimod)的功效与作用有哪些

Etrasimod is a new oral selective sphingosine 1-phosphate (S1P) receptor modulator developed by Pfizer.

Indications for Etrasimod

It is suitable for the treatment of moderately to severely active ulcerative colitis in adults.

Itrimod provides a new treatment option for patients who have had an inadequate response, loss of response, or intolerance to traditional treatments (such as aminosalicylic acid drugs, corticosteroids, immunosuppressants), or biologic agents.

Mechanism of action of Etrasimod

1. Highly selective effect on S1P receptors

Itramod is an S1P receptor modulator that can It binds to S1P receptor subtypes 1, 4, and 5 (S1P₁, S1P₄, S1P₅) with high affinity, but has extremely low activity on S1P₃ receptors (25 times lower than the Cmax at the recommended dose) and no activity on S1P₂ receptors. This selectivity is the basis for its efficacy and reduction of certain side effects, such as bradycardia.

2. Lymphocyte retention effect

Itramod can partially and reversibly block the ability of lymphocytes to migrate from lymphoid tissues (such as lymph nodes) to peripheral blood, leading to a decrease in peripheral blood lymphocyte count and reducing the recruitment of lymphocytes to intestinal inflammation sites, thereby reducing the immune inflammatory response of the intestinal mucosa and promoting tissue repair and healing.

3. Multi-pathway immune regulation

In addition to lymphocytes, S1P receptors are also expressed on other immune cells (such as dendritic cells, macrophages) and non-immune cells (such as endothelial cells, smooth muscle cells). Itramod may regulate immune response and vascular function through multiple pathways, and comprehensively exert anti-inflammatory and tissue protective effects.

The pictures come from public channels (such as the official website of the FDA, the official website of the original drug manufacturer, etc.) and are for reference only.

Medication Guide for Etrasimod

1. Pre-treatment screening

Before starting treatment with Etrasimod, obtain a recent (i.e. within 6 months or after stopping previous ulcerative colitis treatment) complete blood count (CBC), including lymphocyte count.

Obtain a baseline electrocardiogram (ECG) to determine if there are pre-existing cardiac conduction abnormalities; a cardiologist's opinion should be sought in patients with certain preexisting conditions.

Get recent (i.e., within the past 6 months) aminotransferase and bilirubin levels.

Perform baseline fundus evaluation, including macular examination, before and after starting itrimod therapy.

Perform a skin examination before or soon after starting treatment with istrimod. Promptly evaluate any suspicious skin lesions.

Review the patient's current or past medications and determine if the patient is taking any medications that may slow the heart rate or reduce atrioventricular conduction. The possibility of unintentional additive immunosuppression should be considered before initiating treatment with istrimod in patients receiving antineoplastic agents, immunomodulators, or noncorticosteroid immunosuppressive drugs.

VZV antibody testing is performed in patients without a confirmed history of varicella (chickenpox) or complete varicella-zoster virus (VZV) vaccination records before starting treatment with istrimod.

Update vaccinations according to current immunization guidelines before initiating treatment with istrimod. If live attenuated vaccines are required, administer them at least 4 weeks before starting treatment with istrimod.

2. Patient monitoring

Monitor the infection during treatment with istrimod and within 5 weeks after discontinuation of treatment.

For patients receiving concurrent immunosuppressive therapy, monitor for infectious complications during treatment with istrimod and for 5 weeks after the last dose.

Monitor blood pressure during treatment with istrimod.

Perform fundus evaluation (including macular examination) regularly during treatment with istrimod and at any time if any changes in vision occur.

Perform spirometry assessment of respiratory function during treatment with istrimod if clinically indicated.

Perform skin examinations in all patients shortly after starting treatment with istrimod and periodically thereafter, especially in patients with risk factors for skin cancer. Monitor for suspicious skin lesions.

Monitor for the development of immune reconstitution inflammatory syndrome (IRIS) in patients who develop progressive multifocal leukoencephalopathy (PML) while discontinuing itridimod.

3. Dosage

Take orally once a day, 2mg each time.

4. Administration method

Take orally once a day, and the tablet can be swallowed whole with a meal or on an empty stomach.

5. Treatment of missed doses

If a dose of istrimod is missed, the missed dose should be skipped and administration should be resumed at the next scheduled time.

6. Medication for special groups

(1) Hepatic insufficiency

Patients with mild to moderate hepatic insufficiency (Child-Pugh class A or B) do not need to adjust the dose.

Not recommended for patients with severe hepatic insufficiency (Child-Pugh C class).

(2), Renal insufficiency

There is currently no specific dosage recommendation.

(3) Elderly patients

There are currently no specific dosage recommendations.