①. Clinical efficacy of bexarotene soft capsules
In the first study, patients with early-stage cutaneous T-cell lymphoma who were unresponsive to or intolerant to at least two treatments took 300 mg of this product daily. /m2, 15 of 28 patients (54) achieved full or partial response (improvement of at least 50 or above), while the response rate in the higher dose group was 10/15 (67). In addition, 300mg/day Two patients in the m2 group relapsed within 25 weeks.
In the second study, among 94 patients with advanced cutaneous T-cell lymphoma who had failed at least one systemic treatment, 25 of 56 patients received this product at 300 mg/m2 per day ( 45) obtained a response, and another 35 patients received a higher dose of this product, and 21 patients (55) obtained a response; 9 of the patients who responded in the low-dose group relapsed after a median time of 19 weeks.
In the study, ***84 patients received this product at 300 mg/m2 per day, of which 3 patients (4) achieved complete responses and 40 patients (48) achieved partial responses; in the high-dose group Among them, the complete response rate was 9/53 cases (17).
Bexarotene soft capsules have promising prospects as a combination of bioactive preparations and chemotherapy drugs. Currently, Ligand Pharmaceuticals in the United States is conducting trials to evaluate the efficacy of bexarotene and traditional chemotherapy drugs in non-small cell lung cancer. In addition, bexarotene can induce apoptosis in malignant cell lines and plays a role in chemoprevention. The preventive and therapeutic effects of bexarotene in lung cancer are currently being verified.
Forty-three patients with stage IV lung cancer were given a combination of bexarotene, cisplatin, and vinorelbine at a total of 400 mg/m2/day, and the patient achieved a response in 18.6 days.
Phase II and III clinical trials of this drug on breast cancer, psoriasis and other symptoms. The drug has been listed as a new drug in development to treat psoriasis.
148 patients with advanced breast cancer (multi-center study) took this product at 200mg/m2/day, and all patients achieved a response after 8-10 weeks.
50 patients with moderate to severe psoriasis (multi-center study) took this product at 35-240 mg/m2/day. After 12-24 weeks of treatment, 46 patients showed >50% improvement.
②. Clinical efficacy of bexarotene gel:
Bexarotene gel is used to treat patients with early-stage cutaneous T-cell lymphoma who are unresponsive or intolerant to other treatments: In a phase I/II clinical study involving 67 CTCL patients, bexarotene gel was applied topically for at least 4 weeks. 63 (42) patients showed efficacy, and 50 patients had clinical symptoms improved. 21 patients (13) were completely effective. Moderate improvement in localized skin lesions, including erythema, raised plaques, scaling, and pruritus, generally occurred 24 weeks after the start of dosing. The median time to onset of action was 20 weeks (range, 4-86 weeks). The average duration of treatment was 315 days, and the longest duration of treatment was 4.25 years and still under treatment. The median duration of efficacy was 428 days, the shortest was 2 months, and the range was 57-428 days. Bexarotene gel at therapeutic concentrations was shown to be well tolerated locally by 87 (58) patients. Side effects mainly occur at the site of use and are mild. No serious side effects were reported, including rash (73), itching (33), and pain (burning sensation at the application site 24).
In a phase III clinical trial (multi-center), among 50 patients with refractory early-stage cutaneous T-cell lymphoma in the United States, the effective rate of bexarotene gel was 44 (8 were completely effective) . The mid-term treatment time is 165 days, and the longest treatment time is 687 days. Side effects included rash (72), itching (32), pain at the application site (22), skin disorders (16), and contact skin irritation (12).
The I/II clinical trial of bexarotene gel in patients with cutaneous T-cell lymphoma combined with mycosis fungoides achieved efficacy on 11/27 (41), and the patient had a great response to the product. Well tolerated.
In the United States, bexarotene gel was used in a phase II clinical trial on patients with Kaposi's sarcoma or mycosis fungoides, and 15 patients achieved a response.
Bexarotene gel for refractory tinea manuum: Hand dermatitis is receiving increasing attention from the pharmaceutical industry. Currently, there are no treatments specifically approved for this indication, and available treatment options are limited to emollients and topical or oral corticosteroids, cyclosporine, phototherapy, or radiation therapy for severe cases. However, the disease is quite common, with a prevalence of 6 to 11 in Northern Europe. Ligand is planning a Phase II/III clinical trial of bexarotene(1) gel for topical treatment of refractory tinea manuum. Its Phase I/II clinical trial looked at 55 patients with severe long-term hand dermatitis who received topical bexarotene(1) gel alone, topical bexarotene(1) gel plus mometasone furoate, and Comparison of the efficacy of topical bexarotene (1) gel plus hydrocortisone. The results showed that bexarotene(1) gel plus mometasone was the most effective, with physician fixed assessment (PSA) response rates (at least 90 improvement) and PGA response rates (at least 50 improvement) of 46 and 77, respectively. Bexarotene (1) gel alone was less effective (39 and 79 for PSA and PGA respectively). and in combination with cortisone (21 and 50, respectively). It is believed that bexarotene gel has a significant improvement effect on severe hand dermatitis.
Bexarotene gel should be used in patients with psoriasis: UVB light therapy is an FDA-approved method to treat psoriasis, and this method is not effective on thick scales. Bexarotene (1) gel It can make thick scales thinner, allowing ultraviolet rays to pass through effectively and have an inhibitory effect. The combined treatment of UBV and bexarotene (1) gel is expected to improve the efficacy. Bexarotene gel is an FDA-approved topical treatment for T-cell lymphoma and is in clinical trials for the treatment of psoriasis. 1. When bexarotene gel plus NBUBV is used to treat the injured area, the meaningful clinical improvement rate is 67.6; when blank gel is added to NBUBV to treat the injured area, the improvement rate is 48.2. Because the damage area of ??the medical records used was small, the non-statistical parametric Wilcoxon rank-sum test was used to analyze the difference in scores between the two groups. 1. The efficacy score of bexarotene gel plus NBUBV was higher than that of the blank gel control group, with statistical significance (P=0.04). After treatment, the plaque bulge, erythema, and hardening of the lesions were greatly reduced, and the side effects were mild, including rash and Skin irritation. Further clinical studies have been approved.
Bexarotene has a very short drug half-life, which prevents the drug from accumulating in the body. Oral soft capsules have the characteristics of high bioavailability, safe sealing, precise content, and beautiful appearance. The gel acts directly on the diseased skin and is non-greasy, easy to apply, safe to use and convenient to administer.
(4) This product has not applied for a Chinese patent and does not have administrative protection