10 OctLentaron Breast Cancer Treatment Assistant

Introduction about Lentaron

Lentaron which you can also call formestane is classified as a selective irreversible steroidal aromatase inhibitor. This agent is structurally a derivative of androstenedione, differing from this well known prohormone only by the addition of a 4-hydroxyl group. This group, however, is responsible for causing an irreversible attachment between formestane and aromatase when the two come into contact with each other. This means that formestane will bond with the enzyme and never let it go, permanently deactivating it as a result. The enzyme will need to be replaced, through normal attrition, before the body will recover its lost estrogen synthesizing capacity. This may take several days or more following cessation of therapy. Given this mode of action, formestane is also referred to as a “suicide” aromatase inhibitor, as the drug essentially sacrifices itself in the process of blocking estrogen conversion. As a class of drugs, aromatase inhibitors are used (off-label) by male bodybuilders and athletes to prevent the estrogenic side effects of certain anabolic/androgenic steroids, and to increase fat loss and muscle definition while dieting.

Because of its potent estrogen-suppressing action, formestane has been used clinically to treat breast cancer patients in a number of countries including England, Germany, Switzerland, Spain, Australia, New Zealand, Italy, and Malaysia. It has been shown to be an effective option as a second line of defense after tamoxifen, an estrogen receptor antagonist, has failed to elicit a positive response with patients, and produces an overall response statistically similar to tamoxifen when administered as the first-line therapy. In terms of overall potency, formestane is not as strong as the selective third generation inhibitors like Arimidex (anastrozole) or Femara (letrozole). One study, for example, notes a 79% level of suppression of estrogen levels with 4 weeks use of Arimidex 1 mg daily (on par with levels noted with Femara use), but only a 58% level of suppression with intramuscular formestane injections (250 mg every two weeks)¹. But next to estrogen receptor antagonists like Clomid (clomiphene citrate) and Nolvadex (tamoxifen citrate), formestane is significantly more effective at blocking the effects of estrogen in the body.

Side Effect of Lentaron

The side effects which accompany Lentaron use are also those that are common to other AI drugs including fatigue, mood swings, depression, joint pain, hot flashes, headaches, swelling of the arms and legs, and high blood pressure. AIs also suppress HDL (good) cholesterol levels, and may decrease bone density increasing susceptibility to osteoporosis, fractures and breaks.

Administration of Lentaron

Formestane is indicated for the treatment of advanced breast cancer in postmenopausal women. The recommended dosage is 250 mg by intramuscular injection (buttock) every two weeks. Although not a medically approved form of the drug, studies have demonstrated that a similar level of estrogen suppression can also be achieved with oral use of formestane. Due to poor bioavailability, however, the dose needed is around 250 mg per day . When used (off-label) to mitigate the estrogenic side effects of anabolic/androgenic steroid use or increase muscle definition, male athletes and bodybuilders often take 250 mg every two weeks by injection, or 250 mg per day orally.