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| Primary information |
|---|
| ID | 10269 |
| Therapeutic ID | Th1039 |
| Protein Name | Lutropin alfa |
| Sequence | >Th1039_Lutropin_alfa
APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS
|
| Molecular Weight | 30000 |
| Chemical Formula | C1014H1609N287O294S27 |
| Isoelectric Point | 8.44 |
| Hydrophobicity | -0.063 |
| Melting point | 55 |
| Half-life | approximately 18 hours |
| Description | Lutropin alfa is a recombinant human luteinizing hormone produced in yeast with 2 subunits, alpha = 92 residues, beta = 121 residues. It is a heterodimeric glycoprotein. Each monomeric unit is a glycoprotein molecule. In females, an acute rise of LH(LH surge) triggers ovulation and the development of the corpus luteum. In males, it stimulates Leydig cell production of testosterone. Lutropin alfa was the first and only recombinant human form of luteinizing hormone (LH) developed for use in the stimulation of follicular development. |
| Indication/Disease | For treatment of female infertility |
| Pharmacodynamics | Used to facilitate female conception, lutropin alfa performs the same actions as luteinizing hormone, which is normally produced in the pituitary gland. Lutropin is usually given in combination with follitropin alfa. In females, a LH surge about halfway through the menstrual cycle triggers the onset of ovulation. LH also induces the ovulated follicle to become a corpus luteum, which then secretes progesterone. |
| Mechanism of Action | Binds to the luteinizing hormone receptor which then activates adenylate cylcase through G protein mediation. Adenylate cyclase then activates many other pathways leading to steroid hormone production and other follicle maturation processes. |
| Toxicity | Lutropin alfa is not indicated for people under 16 and over 60, pregnant and lactating women, patients with uncontrolled thyroid and adrenal failure, patients with active, untreated tumours of the hypothalamus and pituitary gland, and in any patient with a condition that makes a normal pregnancy possible such as primary ovarian failure or fibroid tumors of the uterus. |
| Metabolism | <5% of dose excreted renally as unchanged drug. |
| Absorption | bioavailability is 56% |
| 10 L |
| Clearance | 2-3 L/h [healthy female following subcutaneous administration]. Total body clearance is approximately 2 to 3 L/h with less than 5 percent of the dose being excreted unchanged renally. |
| Categories | Genito Urinary System and Sex Hormones, Gonadotropins |
| Patents Number | US5767251 |
| Date of Issue | 16-Jun-1998 |
| Date of Expiry | 16-Jun-2015 |
| Drug Interaction | Other drugs may interact with lutropin alfa, including prescription and over-the-counter medicines, vitamins, and herbal products |
| Target | Lutropin-choriogonadotropic hormone receptor |
| Brand Name | Luveris |
| Company | Serono, Merck Europe B.V. |
| Brand Description | Serono, Merck Europe B.V. |
| Prescribed For | Luveris is used together with follitropin alfa to treat infertility in women with LH deficiency. |
| Chemical Name | NA |
| Formulation | One vial contains 75 IU of lutropin alfa (recombinant human Luteinising Hormone {r-hLH}) and following excipeint is present; Powder:Sucrose,Disodium phosphate dihydrate,Sodium dihydrogen phosphate monohydrate,Polysorbate 20,Phosphoric acid, concentrated ( |
| Physical Appearance | White lyophilised pellet withg clear colourless solvent to make solution |
| Route of Administration | Subcutaneous (Subcutaneous) administration |
| Recommended Dosage | It is recommended that 75 IU Luveris be concomitantly administered subcutaneously with 75 IU to 150 IU Gonal-f as two separate injections in the initial treatment cycle |
| Contraindication | Hypersensitivity |
| Side Effects | Nausea, stomach pain, diarrhea, constipation, gas; pelvic pain, menstrual cramps; breast pain; headache; pain or irritation where the injection was given; tired feeling; or cold symptoms such as stuffy nose, sneezing, sore throat. |
| Useful Link 1 | Link |
| Useful Link 2 | NA |
| Remarks | NA |