EXTENDED-RELEASE FORMULATIONS OF HUMAN CHORIONIC GONADOTROPIN (HCG)

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madman

Super Moderator
I. BACKGROUND

Human chorionic gonadotropin (hCG) is a hormone produced by the syncytiotrophoblast cells of the human placenta and gonads. hCG interacts with the luteinizing hormone/choriogonadotropin receptor (LHCGR) (also known as lutropin/choriogonadotropin receptor (LCGR) or luteinizing hormone receptor (LHR) found in the gonads of both genders.

The action of hCG is similar to that of pituitary luteinizing hormone (LH), in that:
both hormones stimulate the production of testosterone and other steroid hormones by the Leydig cells of the testis and both hormones stimulate the production of progesterone by the corpus luteum of the ovary.

During fetal development, hCG produced by the placenta stimulates the fetal testes to produce androgens, which are important to normal male sexual development. In the adult, administration of exogenous hCG stimulates testosterone production from the Leydig cells of the testes. For men with hypogonadotrophic hypogonadism, exogenously administered hCG can stimulate the testicular Leydig cells and restore normal testosterone production. Administration of hCG may also stimulate testicular descent in boys with cryptorchidism when no anatomical impediment to descent is present.

In the female, hCG produced by the placenta stimulates the ovary and promotes the maintenance of the corpus luteum during the beginning of pregnancy. This allows the corpus luteum to secrete the hormone progesterone during the first trimester. Progesterone enriches the uterus with a thick lining of blood vessels and capillaries so that it can sustain the growing fetus.

During the normal menstrual cycle, LH participates with FSH in the development and maturation of the normal ovarian follicle, and the mid-cycle LH surge triggers ovulation. In adult females, clinical administration of exogenous hCG can substitute for an LH surge. For women undergoing in vitro fertilization, hCG is extensively used parenterally for final maturation induction. In the presence of one or more mature ovarian follicles, ovulation can be triggered by the administration of hCG. In addition, hCG is sometimes used to enhance the production of progesterone for clinical purposes during treatment for infertility.

As the most abundant biological source is women who are presently pregnant, some organizations collect urine from pregnant women to extract hCG for pharmaceutical use, in dosage forms marketed under the trade names Novarel" and Pregnyl®. Recombinant hCG is produced through Chinese hamster ovary (CHO) cells and commercially available in a dosage form marketed under the trade name Ovidrel·".

Current commercially available dosage forms of hCG are limited to intramuscular (IM) or subcutaneous (SC) injectable forms which raise serum hCG levels to therapeutic levels over a short period of time.

Frequent injections are required for several clinical applications where sustained dosing of hCG is needed. These applications include but are not limited to the treatment of hypogonadotrophic hypogonadism and stimulation of progesterone production for female fertility.
There is a need in the art for extended-release dosage forms of hCG. The present invention satisfies this need.



II. SUMMARY

The present disclosure relates to the long-felt need in the art for extended-release human chorionic gonadotropin (hCG) formulations. In particular, the present disclosure is directed to hCG dosage forms having extended-release profiles. In some embodiments, the hCG dosage forms exhibit release profiles of between about 1 week and about 2 months. In other embodiments, the hCG dosage forms described herein can have extended-release profiles between about 1 week and about 6 months.

In some aspects, the extended-release hCG dosage form comprises hCG encapsulated in a microsphere. In further aspects, the microsphere is formed by a copolymer. In still further aspects, the copolymer is a block copolymer or a multi-block copolymer. In such aspects, the block copolymer may comprise or alternatively consists essentially of, polyethylene glycol (PEG) or a PEG-containing polymeric block and one or more other polymeric blocks.

hCG extended-release formulations described herein may be useful in a variety of treatments relating to hormone therapy, including but not limited to treatment for infertility and pituitary gland disorders.
Thus, further aspects of the disclosure relate to methods of administering the extended-release hCG formulations described herein, as well as methods of treatment employing the extended-release hCG formulations described herein. Such methods include treatments for fertility and pituitary gland defects. Further methods disclosed herein include the treatment of breast cancer. In some embodiments, the treatment is for existing breast cancer in nulliparous women. In some embodiments, the women are about age 25 or younger.





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Applicants
  • INNOCORE TECHNOLOGIES HOLDING B.V. [NL]/[NL]
  • MHB LABS, INC. [US]/[US]

Inventors
  • ZUIDEMA, Johan
  • STEENDAM, Rob
  • ARAUJO, Joana Catarina Ribeiro
  • KACKER, Ravi
  • MORGENTALER, Abraham
 

Attachments

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Defy Medical TRT clinic doctor

madman

Super Moderator

API
SynBiosys is a sustained release technology using several monomers to form a biodegradable polymer matrix in which APIs can be entrapped. When brought in an aqueous environment, the polymers swell and gradually release the APIs by diffusion. Release time can be regulated from days up to several months.

*Protein & Antibodies

*Peptides
*SmallMolecules


Polymer technologies
InnoCore has two patented sustained release technologies that serve as a platform for obtaining advanced long-acting injectable (LAI) formulations of pharmaceutical ingredients. The SynBiosys® and InGell® polymers are biodegradable and bioresorbable in which APIs can be entrapped. The long-acting release mechanism of drugs with SynBiosys® microspheres is based upon diffusion whereas the InGell® gels erode completely via surface erosion. Optionally, PLGA could be used as a drug carrier in microspheres although with limited patent protection.

*Synbiosys
*Ingell

*PLGA


Drug carriers

InnoCore’s technologies can be applied in several administration forms. Our SynBiosys® platform is compatible with state-of-the-art depot formulation technologies, like microspheres, microrods, microparticles, nanoparticles, and in-situ forming implants or gels. The technology is also suitable for implants, fleece’s, and for spray coating of implants, like coronary stents and other vascular devices. The InGell® technology is an advanced injectable gel drug depot system, offering unparalleled retention and release of active pharmaceutical ingredients from a soft, localized drug depot. The InGell technology is available as a water-borne gel (hydrogel consisting of 75-90% of buffer) and a water-free gel (100% pure polymer, LQP).

*Microspheres
*Gell
*Implant
*Nanospheres
*Coating

*Other


Sustained release
In today's health care industry, sustained drug delivery has become key in pharmaceutical product development. Innovative sustained release technologies allow for increased performance of new and existing pharmaceutical compounds. Patients benefit from the enhanced efficacy of pharmaceutical products and from the reduction of side effects.

 

madman

Super Moderator

A brief introduction of Innocore Pharmaceuticals, a biopharmaceutical drug delivery company specialized in the development of long-acting drug delivery products for the treatment of chronic diseases. This video was made for our nomination for the Groningen Entrepreneurial Award 2017.
 

Nelson Vergel

Founder, ExcelMale.com
Very interesting! Dr Morgentaler mentioned this two years ago in a video but did not reply to my emails inquiring about it. He may be an investor.
 

madman

Super Moderator

*Another consideration is long-lasting treatments that are not associated with side effects such as infertility and testicular atrophy. One promising idea is a slow-release human chorionic gonadotropin formulation, currently in development, designed to boost endogenous serum T for at least 2 months
 
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