==== Reference: Usmani SS, Bedi G, Samuel JS, Singh S, Kalra S, Kumar P, et al. (2017) THPdb: Database of FDA-approved peptide and protein therapeutics. PLoS ONE 12(7) e0181748.====

Detailed description page of THPdb

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1639 details
Primary information
ThPP IDTh1144
Therapeutic Peptide/Protein NameFollitropin alpha
SequenceN.A. view full sequnce in fasta
Functional ClassificationIb
Molecular WeightN.A.
Chemical FormulaN.A.
Isoelectric PointN.A.
HydrophobicityN.A.
Melting Point (℃)N.A.
Half LifeN.A.
DescriptionRecombinant (CHO cell derived) human follicle stimulating hormone (FSH). It consists of two non-covalently linked, non-identical glycoproteins designated as the alpha (92 amino acids)- and beta (111 amino acids)- subunits. The alpha subunit is glycosylated at N51 and N78 while the beta subunit is glycosylated at N7 and N24. Follitropin alpha was the world's first recombinant human FSH preparation. The term “alpha” differentiates it from another recombinant human FSH product that was marketed later as follitropin beta. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate than beta but with significantly higher estradiol (E2) levels. The amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side-chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH.
Indication/DiseaseIn women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF)
PharmacodynamicsThe main pharmacodynamic parameters are serum inhibin, estradiol and total follicular volume with daily injections of follitropin. The quickest response was noticed with serum inhibin, which declined rapidly after discontinuation. Follicular growth showed late response and continued even after discontinuation of the drug and after decline of the serum concentrations. Thus follicular growth was better correlated with serum inhibin and estradiol rather than peal levels of the drug. It should be noted that there is great inter-individual variability
Mechanism of ActionFollitropin is important for spermatogenesis, gonadal steroid production and follicule growth and maturation
ToxicityHeadaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers
MetabolismN.A.
Absorption74%.
Volume of DistributionN.A.
ClearanceN.A.
CategoriesN.A.
Patents NumberN.A.
Date of IssueN.A.
Date of ExpiryN.A.
Drug InteractionN.A.
TargetN.A.
Information of corresponding available drug in the market
Brand NameGonal-f RFF
CompanyEMD SERONO
Brand DiscriptionGonal-f RFF (follitropin alfa for injection) is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the α- and β-subunits. The α- and β-subunits have 92 and 111 amino acids, respectively, and their primary and tertiary structure are indistinguishable from those of human follicle stimulating hormone. Recombinant FSH production occurs in genetically modified Chinese Hamster Ovary (CHO) cells cultured in bioreactors. Purification by immunochromatography using an antibody specifically binding FSH results in a highly purified preparation with a consistent FSH isoform profile, and a high specific activity. The biological activity of follitropin alfa is determined by measuring the increase in ovary weight in female rats. The in vivo biological activity of follitropin alfa has been calibrated against the first International Standard for recombinant human follicle stimulating hormone established in 1995 by the Expert Committee on Biological Standards of the World Health Organization. Gonal-f RFF (follitropin alfa injection) contains no luteinizing hormone (LH) activity. Based on available data derived from physico-chemical tests and bioassays, follitropin alfa and follitropin beta, another recombinant follicle stimulating hormone product, are indistinguishable.
Prescribed forovulation and pregnancy in the oligo-anovulatory infertile patient in whom the cause of infertility is functional and not due to primary ovarian failure, development of multiple follicles in the ovulatory patient participating in an Assisted Reproductive Technology (ART) program.
Chemical NameN.A.
FormulationEach Gonal-f RFF single-dose vial is filled with 82 IU (6 µg)follitropin alfa to deliver 75 IU (5.5 µg) follitropin alfa and contains 30 mg sucrose, 1.11 mg dibasic sodium phosphate dihydrate, 0.45 mg monobasic sodium phosphate monohydrate, 0.1 mg methionine, and 0.05 mg polysorbate 20. Phosphoric acid and/or sodium hydroxide may be used prior to lyophilization for pH adjustment. Vials are reconstituted with Sterile Water for Injection, USP.
Physcial AppearnceGonal-f RFF (follitropin alfa injection) is a sterile, lyophilized powder intended for subcutaneous injection after reconstitution.
Route of AdministrationSubcutaneous Injection
Recommended Dosage300 IU per day
ContraindicationPrior hypersensitivity to recombinant FSH preparations or one of their excipients, High levels of FSH indicating primary ovarian failure., Uncontrolled thyroid or adrenal dysfunction, An organic intracranial lesion such as a pituitary tumor, Sex hormone dependent tumors of the reproductive tract and accessory organs, Abnormal uterine bleeding of undetermined origin, Ovarian cyst or enlargement of undetermined origin, Pregnancy.
Side EffectsHeadache, Dizziness, Migraine, Abdominal Pain, Nausea, Flatulence, Diarrhea, Toothache, Dyspepsia, Constipation, Stomatitis Ulcerative, Ovarian Cyst, Reproductive, Female, Ovarian Hyperstimulation, Breast Pain Female, Vaginal Haemorrhage, Gynecological-related pain, Uterine haemorrhage, Sinusitis, Pharyngitis, Rhinitis, Coughing, Injection Site Pain, Injection Site Inflammation, Back Pain, Pain, Fever, Hot Flushes, Malaise, Acne, Micturition Frequency, Cystitis, Infection viral.
Useful Linkhttp://www.rxlist.com/gonal-f-rff-drug.htm http://www.drugs.com/pro/gonal-f-rff.html http://www.webmd.com/drugs/2/drug-91245/gonal-f-rff-pen-subq/details
PubMed ID20238314, 18020563, 20101851
3-D StructureN.A.