1   药品名称

贝卡普勒明 

2  英文名称

Becaplermin 

3   分类

内分泌系统药物 > 糖尿病及胰岛疾病用药物

4   剂型

每支2g，7.5g和15g装，含贝卡普勒明0.01%。

5   贝卡普勒明的药理作用

血小板源生长因子（PDGF）是一种内源生长因子，有PDGF-AA，PDGF-AB，PDGF-BB三种亚型，其中贝卡普勒明（PDGF-BB）保持有PDGF的全部活性，因而与PDGF作用方式类似。贝卡普勒明通过促细胞有丝分裂、促趋化和促蛋白质合成作用，加速创伤的愈合。贝卡普勒明的促有丝分裂作用与PDGF-AB以及胰岛素样生长因子（IGF-1）相似，最大促有丝分裂活性浓度为10ng/mL。贝卡普勒明的促趋化活性仅次于IGF-1。而且贝卡普勒明的作用可以通过与IGF-1合用而得到加强。贝卡普勒明也能显著提高创伤愈合部位肉芽的生长。另外，贝卡普勒明可促进骨的生长，既能提高骨皮质的增长，也能提高骨髓质的补充。

6   贝卡普勒明的药代动力学

贝卡普勒明属局部外用药。在一般使用7µg/cm2的剂量下，贝卡普勒明在血液中几乎无法测到。 每天涂敷足够厚度含贝卡普勒明0.01%凝胶制剂，持续14天，可减轻发生糖尿病溃疡的痛苦。这种日常用药方式只表明贝卡普勒明轻微的全身性吸收。因此，目前几乎没有关于该药的有用药动学数据，同样也没有数据表明人乳中是否存在贝卡普勒明。

7   贝卡普勒明的适应证

用于糖尿病引发的腿足部溃疡的治疗。

8 注意事项

仅限于外用。可能贝卡普勒明在使用过程中会出现局部过敏和刺激，需注意。

9   贝卡普勒明的不良反应

会引起感染，蜂窝组织炎和骨髓炎，但发生率与不使用贝卡普勒明时相似。另外约有2%的患者会出现红斑狼疮样皮疹（erythematous rashes）。

10  贝卡普勒明的用法用量

外涂，用药前先清洁创面，然后将贝卡普勒明薄薄涂在溃疡面上，用生理盐水敷料盖面，用量多少取决于溃疡创伤面的大小，1次/d。

Medically reviewed on March 25, 2018

· Recombinant Human Platelet-Derived Growth Factor B

· rPDGF-BB

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Gel, External:

Regranex: 0.01% (15 g) [contains metacresol, methylparaben, propylparaben]

Regranex

· Growth Factor, Platelet-Derived

· Topical Skin Product

Recombinant B-isoform homodimer of human platelet-derived growth factor (rPDGF-BB) which enhances formation of new granulation tissue, induces fibroblast proliferation and differentiation to promote wound healing; also promotes angiogenesis.

Diabetic ulcers: Adjunctive treatment of lower extremity diabetic neuropathic ulcers that extend into the subcutaneous tissue or beyond and have an adequate blood supply.

Limitations of use: Efficacy has not been established for pressure and venous stasis ulcers; has not been evaluated for diabetic neuropathic ulcers that do not extend through the dermis into subcutaneous tissue (stage I or II, International Association of Enterostomal Therapy [IAET] staging classification) or ischemic diabetic ulcers.

Known neoplasm(s) at the site(s) of application

Diabetic ulcers (lower extremity): Topical: Apply appropriate amount of gel once daily with a cotton swab, tongue depressor, or similar tool, as a coating over the ulcer. The amount of becaplermin to be applied will vary depending on the size of the ulcer area.

Note: If the ulcer does not decrease in size by ~30% after 10 weeks of treatment or complete healing has not occurred in 20 weeks, continued treatment with becaplermin gel should be reassessed.

Estimation of gel requirement: To calculate the length of gel applied to the ulcer, measure the greatest length of the ulcer by the greatest width of the ulcer. Tube size and unit of measure will determine the formula used in the calculation. Recalculate amount of gel needed every 1 to 2 weeks, depending on the rate of change in ulcer area.

Centimeters:

15 g tube: [ulcer length (cm) x width (cm)] divided by 4 = length of gel (cm)

2 g tube: [ulcer length (cm) x width (cm)] divided by 2 = length of gel (cm)

Inches:

15 g tube: [length (in) x width (in)] x 0.6 = length of gel (in)

2 g tube: [length (in) x width (in)] x 1.3 = length of gel (in)

Refer to adult dosing.

Diabetic ulcers (lower extremity): Adolescents ≥16 years: Refer to adult dosing

There are no dosage adjustments provided in the manufacturer's labeling. However, dosage adjustment unlikely due to low systemic absorption.

There are no dosage adjustments provided in the manufacturer's labeling. However, dosage adjustment unlikely due to low systemic absorption.

For topical use; not for oral, ophthalmic, or intravaginal use. Squeeze appropriate amount of gel onto clean measuring surface (eg, wax paper), spread onto entire ulcer area in a thin, continuous layer ~1/16 inch thick. Cover with saline moistened dressing; leave dressing in place ~12 hours. After 12 hours, remove dressing, rinse with saline or water to remove residual becaplermin gel and cover with saline moistened dressing (without becaplermin gel) for remainder of the day. Continue use once daily until ulcer is completely healed.

Refrigerate at 2°C to 8°C (36°F to 46°F); do not freeze. The following stability information has also been reported: May be stored at room temperature for up to 6 days (Cohen, 2007).

There are no known significant interactions.

1% to 10%: Dermatologic: Erythematous rash (2%)

<1%, postmarketing, and/or case reports: Connective tissue disorder (excessive granulation tissue), dermal ulcer (with or without tunneling), erythema (with purulent discharge), local pain

Malignancy:

An increased rate of mortality secondary to malignancy was observed in patients treated with 3 or more tubes of becaplermin in a postmarketing retrospective cohort study. Becaplermin should only be used when the benefits can be expected to outweigh the risks. Becaplermin should be used with caution in patients with known malignancy.

Concerns related to adverse effects:

• Application site reactions: Sensitization or irritation of skin may occur; may be due to parabens or m-cresol. Interruption or discontinuation of treatment should be considered; further evaluation (eg, patch testing) may be necessary.

• Malignancy: [U.S. Boxed Warning]: An increased rate of mortality secondary to malignancies was observed in a postmarketing retrospective cohort study of patients treated with ≥3 tubes of becaplermin. Becaplermin should only be used when the benefits can be expected to outweigh the risks. Use with caution in patients with known malignancy. Malignancies of varying types have been reported; all were remote from the becaplermin treatment site.

Other warnings/precautions:

• Appropriate use: For external use only; do not use in wounds that close by primary intention. Effects on exposed joints, tendons, ligaments and bone have not been established.

Ulcer volume (pressure ulcers); wound area; evidence of closure; drainage (diabetic ulcers); signs/symptoms of toxicity (erythema, local infections)

Animal reproduction studies have not been conducted.

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Have patient report immediately to prescriber severe skin irritation (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.