Stapokibart Injection 司普奇拜单抗注射液 ，司他泊芬注射液

Kangyueda® (sepkizumab) was independently developed by Conoya. [3-4] It is the first IL-4Rα antibody drug approved for marketing in China and the second in the world. [3-4]
The first dose of Kangyueda® (sepkizumab) can quickly relieve itching symptoms after one day of treatment; after two weeks of treatment, it has a strong improvement effect on skin lesions in all parts of the body. [5] After 52 weeks of monotherapy, Kangyueda® (sepkizumab) can achieve the “double 9 reachable” treatment goal of continuous improvement of skin lesions – that is, more than 90% of patients achieve an improvement of more than 75% in the area and severity index of eczema (EASI-75), and nearly 80% of patients achieve an improvement of more than 90% in the area and severity index of eczema (EASI-90). [5] Kangyueda® (sepkizumab) can effectively reduce the risk of recurrence and show good safety and tolerability. [5] The product can effectively reduce the risk of recurrence. The recurrence rate after 52 weeks of treatment is only 0.9%, the recurrence rate after 8 weeks of discontinuation is only 0.9%, and the incidence of conjunctivitis is only 5.3%. [8]
Currently, the application for marketing authorization of sepkizumab for the treatment of moderate to severe atopic dermatitis in adults was approved by the National Medical Products Administration on September 12, 2024 [6], and its application for marketing authorization for the treatment of chronic sinusitis with nasal polyps [5] and seasonal allergic rhinitis [5] has been accepted. [3]
On December 25, 2024, Kangyueda (sepkizumab injection), the first domestic biological agent for the treatment of chronic sinusitis with nasal polyps, was prescribed for the first time in the country at Beijing Tongren Hospital affiliated to Capital Medical University. [9]
On February 7, 2025, Conoya announced that sepkizumab injection was approved for the treatment of seasonal allergic rhinitis. [14]
Specifications

300mg (2ml)/bottle [2]
Ingredients

Active ingredient: Sepkizumab
Sepkizumab is a humanized monoclonal antibody (IgG4 type) targeting interleukin-4 receptor subunit α (IL-4Rα) expressed in Chinese hamster ovary cells, which can inhibit IL-4/IL-13 signaling.

Excipients: sodium acetate, glacial acetic acid, arginine hydrochloride, polysorbate 80 (II) and water for injection. [10]
Dosage and Administration

This product should be prescribed by medical professionals with experience in diagnosing and treating the indication.

Dosage
The initial dose of this product for adults is 600mg (300mg injection twice), followed by 300mg subcutaneous injection once every two weeks.
Patients who do not respond to this product after 16 weeks of treatment for atopic dermatitis should consider stopping treatment. Some patients who partially respond to initial treatment may improve with continued treatment after 16 weeks.
Dosage
This product should be injected subcutaneously once every two weeks. The injection site can be the abdomen, thigh or upper arm, except for the area within 5 cm around the navel.
For the initial dose of 600 mg, two consecutive injections of 300 mg should be given at different injection sites.
It is recommended to rotate the injection site each time the injection is given. This product should not be injected into fragile, damaged or bruised or scarred skin.
Missed medication
If missed medication occurs, the medication should be given as soon as possible.
When patients who take medication every two weeks miss a dose, they should take a supplementary dose within 7 days after the scheduled dose date and then resume the original dosing schedule; if it exceeds 7 days after the scheduled dose date, the medication should be taken as soon as possible and the dosing schedule should be rescheduled to once every two weeks.
Special populations
Elderly patients (≥65 years old)
For elderly patients, it is recommended to use under the guidance of a doctor.
Renal insufficiency
For patients with atopic dermatitis with mild and moderate renal impairment, no dose adjustment is required. There is no data on this product in patients with severe renal impairment and end-stage renal disease with or without dialysis.
Liver damage
There is no data on the use of this product in patients with liver impairment. [10]
Pharmacokinetics
Report

After a single subcutaneous injection of this product in healthy subjects, the blood concentration of each dose group (75 mg, 150 mg, 300 mg, 600 mg) reached peak values ​​within 3 to 14 days.
After multiple doses of this product (600 mg (first dose) + 300 mg Q2W) in patients with moderate to severe atopic dermatitis, the blood concentration was close to steady-state at 12 weeks, and the mean steady-state trough concentrations (±SD) at 12 and 16 weeks were 52.3 (±22.8) and 55.2 (±25.5) μg/mL, respectively.
Distribution
After a single subcutaneous injection of this product, the mean apparent distribution volume of each dose group (75 mg, 150 mg, 300 mg, 600 mg) ranged from 3.64 L to 6.73 L, indicating that the distribution of this product is mainly limited to the blood circulation system.
Biotransformation
This product is a monoclonal antibody that is degraded into small peptides and single amino acids in the human body.
Elimination
This product has two main elimination pathways: IL-4Rα target-mediated elimination and proteolysis. When the in vivo concentration is low, IL-4Rα target-mediated elimination is dominant; when the in vivo concentration is high, proteolysis is dominant. After multiple administrations of the target dose of 600 mg (first dose) + 300 mg Q2W for moderate to severe atopic dermatitis patients, the average apparent clearance was 0.0246 L/h and the average elimination half-life was 12.9 days.
Linear/nonlinear
This product exhibits nonlinear PK characteristics, and the exposure (area under the drug-time curve, AUC) increases with the increase of the single subcutaneous injection dose (75 mg ~ 600 mg) in a manner higher than the dose increase ratio.
Special populations
Gender
Population PK analysis did not find a clinically significant effect of gender on the exposure of this product.
Elderly patients
Population PK analysis did not find a clinically significant effect of age on the exposure of this product.
Hepatic impairment
No specific clinical pharmacology study was conducted to evaluate the effect of hepatic impairment on the PK of this product.
This product is a monoclonal antibody and is not expected to undergo significant liver metabolism and excretion, so no clinical study was conducted to evaluate the effect of hepatic impairment on the PK of this product.
Renal impairment
No specific clinical pharmacology study was conducted to evaluate the effect of renal impairment on the PK of this product.
This product is a monoclonal antibody and is not expected to undergo significant renal excretion, so no clinical study was conducted to evaluate the effect of renal impairment on the PK of this product.
Population PK covariate analysis showed that creatinine clearance (CLCR) had little effect on the exposure of this product.
Weight
The trough concentration of this product was lower in subjects with higher body weight. Population PK analysis showed that body weight had a greater effect on the exposure of this product, with subjects with a body weight of 49 kg (5th quantile) and 88 kg (95th quantile) having exposure changes of +41% to +47% and -42% to -37% respectively relative to typical subjects with a body weight of 67 kg. No significant clinically significant effect of body weight on efficacy was found.
Immunogenicity
As with all therapeutic proteins, this product may be immunogenic.
In patients with atopic dermatitis who received a 600 mg (first dose) + 300 mg Q2W regimen for 16 weeks, the prevalence of anti-drug antibodies was 0.3%, and no neutralizing antibodies were detected in all ADA-positive subjects. The prevalence of anti-drug antibodies in the placebo group was 0.7%, and no neutralizing antibodies were detected. In the continuation study, the prevalence of anti-drug antibodies in adult patients with atopic dermatitis who received long-term treatment with this product (52 weeks) was 2.7%.
The available data show that the prevalence of anti-drug antibodies for this product is low, and the impact of immunogenicity on the PK, efficacy and safety of this product cannot be determined. [10]
Precautions

Hypersensitivity reactions
If systemic hypersensitivity reactions (immediate or delayed) occur, this product should be discontinued immediately and appropriate treatment should be initiated. Rare cases of hypersensitivity reactions have been reported after administration of this product (see [Adverse Reactions]), which occurred within minutes after administration.
Conjunctivitis and keratitis-related events
Patients treated with this product should undergo an ophthalmological examination if they develop conjunctivitis that is not relieved by standard treatment or have signs and symptoms suggestive of keratitis (see [Adverse Reactions]).
Patients with atopic dermatitis with asthma
Patients with moderate to severe atopic dermatitis and asthma who are treated with this product should not adjust or stop their asthma treatment without consulting their doctor. After discontinuation of this product, patients should be carefully monitored for asthma.
Vaccination
When administering this product, live vaccines and live attenuated vaccines should be avoided at the same time, as the clinical safety and efficacy of such practices have not been established. It is recommended that patients should have completed live and live attenuated vaccination according to current immunization guidelines before treatment with this product. There is no clinical data to support more specific guidance on the administration of live or live attenuated vaccines to patients treated with this product.
Sodium content
This product contains less than 1mmol (23 mg) of sodium per 300 mg dose, that is, it is basically “sodium-free”.
Incompatibility In the absence of incompatibility studies, this product should not be mixed with other drugs. [10]