Injectable Peptide Therapy: A Primer for Orthopaedic and Sports Medicine Physicians
Therapeutic peptides are short-chain amino acids that regulate cellular functions and facilitate biochemical processes. In recent years, there has been significant growth in the global market for therapeutic peptides and thus its popularity among ...
Mayfield CK, Bolia IK, Feingold CL et al. — The American journal of sports medicine
Safety and Efficacy of Approved and Unapproved Peptide Therapies for Musculoskeletal Injuries and Athletic Performance
Peptides are short chains of amino acids with a unique pharmacological niche between small-molecule drugs and large proteins. Their use in sports medicine is rapidly expanding, driven by patient demand for accelerated injury recovery and performan...
Mendias CL, Awan TM — Sports medicine (Auckland, N.Z.)
Therapeutic Peptides in Orthopaedics: Applications, Challenges, and Future Directions
Therapeutic peptides are emerging as promising adjuncts in the management of orthopaedic injuries, grounded in their ability to modulate molecular signaling networks central to cellular medicine. By acting on key pathways such as PI3K/Akt, mTOR, M...
Rahman OF, Lee SJ, Seeds WA — Journal of the American Academy of Orthopaedic Surgeons. Global research & reviews
Body composition, hepatic fat, metabolic, and safety outcomes of Tesamorelin, a GHRH analogue, in HIV-associated lipodystrophy: A meta-analysis of randomized controlled trials
HIV-associated lipodystrophy leads to visceral fat accumulation, metabolic complications, body image concerns, medication non-adherence, and increased cardiovascular risks. We thought to assess the effects of Tesamorelin, a synthetic growth hormon...
Badran AS, Helal A, Shata KS et al. — Obesity research & clinical practice
Effects of Tesamorelin on Neurocognitive Impairment in Persons With HIV and Abdominal Obesity
In people with HIV who are virally suppressed with antiretroviral therapy, abdominal obesity (AO) is linked to neurocognitive impairment (NCI), potentially due to visceral adiposity, inflammation, and reduced insulin-like growth factor 1 (IGF-1). ...
Ellis RJ, Vaida F, Hu K et al. — The Journal of infectious diseases
The growth hormone secretagogue receptor 1a agonists, anamorelin and ipamorelin, inhibit cisplatin-induced weight loss in ferrets: Anamorelin also exhibits anti-emetic effects via a central mechanism
This study investigated whether ghrelin mimetics, namely anamorelin and ipamorelin, can alleviate weight loss and inhibition of feeding observed during acute and delayed phases of cisplatin-induced emesis in ferrets. The potential of anamorelin to...
Lu Z, Ngan MP, Liu JYH et al. — Physiology & behavior
Chromatographic-mass spectrometric analysis of peptidic analytes (2-10 kDa) in doping control urine samples
Peptides with a molecular mass between 2 and 10 kDa that are prohibited in elite sports usually require dedicated sample preparation and mass spectrometric detection that commonly cannot be combined with other (lower molecular mass) substance...
Thomas A, Walpurgis K, Thevis M — Journal of mass spectrometry : JMS
Probing for peptidic drugs (2-10 kDa) in doping control blood samples
Bioactive peptides with a molecular mass between 2 and 10 kDa represent an important class of substances banned in elite sports, which has been recognized with an increasing number and variety of substances by anti-doping organizations. Also,...
Thomas A, Thilmany S, Hofmann A et al. — Analytical science advances
Efficacy and safety of tesamorelin in people with HIV on integrase inhibitors
Tesamorelin is the only FDA-approved therapy to treat abdominal fat accumulation in people with HIV (PWH). Phase III clinical trials were conducted prior to the introduction of integrase inhibitors (INSTIs), which are now a mainstay of HIV antiret...
Russo SC, Ockene MW, Arpante AK et al. — AIDS (London, England)
Cationic exchange SPE combined with triple quadrupole UHPLC-MS/MS for detection of GHRHs in urine samples
The use of growth hormone-releasing hormones (GHRHs) is prohibited in sports according to the regulations of the World Anti-Doping Agency (WADA). Considering the complexity of urine samples and the low concentrations at which these analytes should...
Cristea CD, Radu M, Toboc A et al. — Analytical biochemistry
In-house standards derived from doping peptides: Enzymatic and serum stability and degradation profile of GHRP and GHRH-related peptides
Matrix effect and sample pretreatment significantly affect the percentage recovery of peptides in biological matrices, affecting the method robustness and accuracy. To counteract this effect, an internal standard (IS) is used; however, in most cas...
González-López NM, Guerra-Acero-Turizo LM, Blanco-Medina I et al. — Biomedical chromatography : BMC
Online large volume sample staking preconcentration and separation of enantiomeric GHRH analogs by capillary electrophoresis
A capillary electrophoresis method is proposed to analyze the four most well-known growth hormone-releasing hormone (GHRH) analogs that are misused by athletes. Dimethyl-β-cyclodextrin used as a chiral selector allowed, for the first time, t...
Otin J, Tran NT, Benoit A et al. — Electrophoresis
Effect of tesamorelin in people with HIV with and without dorsocervical fat: Post hoc analysis of phase III double-blind placebo-controlled trial
Tesamorelin, a synthetic growth hormone-releasing hormone, is indicated for the reduction of visceral adipose tissue (VAT) in people with HIV. Here, we performed a post hoc analysis of participants receiving tesamorelin for 26 weeks in a phase III...
Rahman F, McLaughlin T, Mesquita P et al. — Journal of clinical and translational science
A potentially effective drug for patients with recurrent glioma: sermorelin
Treatment insensitivity is the main cause of glioma. This study was designed to screen out effective drugs for recurrent gliomas based on the transcriptomics data.
Chang Y, Huang R, Zhai Y et al. — Annals of translational medicine
An antibody-free, ultrafiltration-based assay for the detection of growth hormone-releasing hormones in urine at low pg/mL concentrations using nanoLC-HRMS/MS
This work presents an ultrafiltration-based, validated method for the screening and confirmation of prohibited growth hormone-releasing hormone (GHRH) analogues (sermorelin/CJC-1293, sermorelin metabolite, CJC-1295 and tesamorelin) in urine by nan...
Coppieters G, Deventer K, Polet M et al. — Journal of pharmaceutical and biomedical analysis
Advances in the detection of growth hormone releasing hormone synthetic analogs
The administration of growth hormone releasing hormone (GHRH) and its synthetic analogs is prohibited by the World Anti-Doping Agency (WADA). Although there is evidence of their use, based on admissions and intelligence, they do not appear to have...
Memdouh S, Gavrilović I, Ng K et al. — Drug testing and analysis
Effects of tesamorelin on hepatic transcriptomic signatures in HIV-associated NAFLD
Nonalcoholic fatty liver disease (NAFLD) is a common comorbidity among people living with HIV that has a more aggressive course than NAFLD among the general population. In a recent randomized placebo-controlled trial, we demonstrated that the grow...
Fourman LT, Billingsley JM, Agyapong G et al. — JCI insight
A method for confirming CJC-1295 abuse in equine plasma samples by LC-MS/MS
CJC-1295 is a peptide-based drug that stimulates the production of growth hormone (GH) from the pituitary gland. It incorporates a functional maleimido group at the C-terminus that allows it to covalently bind plasma proteins such as serum albumin...
Timms M, Ganio K, Steel R — Drug testing and analysis
Beyond the androgen receptor: the role of growth hormone secretagogues in the modern management of body composition in hypogonadal males
Male hypogonadism is an increasingly prevalent clinical condition that affects patients' quality of life and overall health. Obesity and metabolic syndrome can both cause and result from hypogonadism. Although testosterone remains the gold standar...
Sinha DK, Balasubramanian A, Tatem AJ et al. — Translational andrology and urology
Effects of tesamorelin on non-alcoholic fatty liver disease in HIV: a randomised, double-blind, multicentre trial
Non-alcoholic fatty liver disease (NAFLD) is a substantial cause of comorbidity in people with HIV and there are no proven pharmacological treatments for the disease in this population. We assessed the effects of tesamorelin on liver fat and histo...
Stanley TL, Fourman LT, Feldpausch MN et al. — The lancet. HIV
An immuno polymerase chain reaction screen for the detection of CJC-1295 and other growth-hormone-releasing hormone analogs in equine plasma
CJC-1295 is a 30 amino acid peptide-based drug that stimulates the release of growth hormone (GH) from the pituitary gland. It is unique among performance-enhancing peptides due to the presence of a reactive maleimidopropionic acid group that cova...
Timms M, Ganio K, Forbes G et al. — Drug testing and analysis
Operation resistance: A snapshot of falsified antibiotics and biopharmaceutical injectables in Europe
Operation Pangea is an annual international week of action combating pharmaceutical crime. In this study, called Operation Resistance, we asked the national agencies in Europe to search for falsified antibiotics and biopharmaceutical injectables (...
Venhuis BJ, Keizers PH, Klausmann R et al. — Drug testing and analysis
Netnography of Female Use of the Synthetic Growth Hormone CJC-1295: Pulses and Potions
Communal online folk pharmacology fuels the drive for short cuts in attaining muscle enhancement, fat loss, and youthful skin.
Van Hout MC, Hearne E — Substance use & misuse
Efficacy of ipamorelin, a ghrelin mimetic, on gastric dysmotility in a rodent model of postoperative ileus
Delayed gastric emptying is a common disorder with few effective therapeutic options. The goal of this study was to investigate whether ipamorelin, a synthetic peptidomimetic that acts on the ghrelin receptor, accelerates gastric emptying in a rod...
Greenwood-Van Meerveld B, Tyler K, Mohammadi E et al. — Journal of experimental pharmacology
Qualitative identification of growth hormone-releasing hormones in human plasma by means of immunoaffinity purification and LC-HRMS/MS
The use of growth hormone-releasing hormones (GHRHs) is prohibited in sports according to the regulations of the World Anti-Doping Agency (WADA). The aim of the present study was to develop a method for the simultaneous detection of four different...
Knoop A, Thomas A, Fichant E et al. — Analytical and bioanalytical chemistry
Expanded test method for peptides >2 kDa employing immunoaffinity purification and LC-HRMS/MS
Bioactive peptides with an approximate molecular mass of 2-12 kDa are of considerable relevance in sports drug testing. Such peptides have been used to manipulate several potential performance-enhancing processes in the athlete's body and include ...
Thomas A, Walpurgis K, Tretzel L et al. — Drug testing and analysis
Prospective, randomized, controlled, proof-of-concept study of the Ghrelin mimetic ipamorelin for the management of postoperative ileus in bowel resection patients
Postoperative ileus is a significant clinical challenge lacking effective management strategies. Ghrelin-receptor stimulation has promotility effects in the upper and lower gastrointestinal tract.
Beck DE, Sweeney WB, McCarter MD et al. — International journal of colorectal disease
Population pharmacokinetic analysis of tesamorelin in HIV-infected patients and healthy subjects
Tesamorelin is a synthetic analogue of growth hormone-releasing factor (GRF), which increases basal and pulsatile growth hormone (GH) secretion and subsequently increases insulin-like growth factor (IGF)-1. Limited information is available about t...
González-Sales M, Barrière O, Tremblay PO et al. — Clinical pharmacokinetics
Growth Hormone Releasing Hormone Analog Sermorelin: Clinical Applications and Pharmacology
Review of sermorelin as a GHRH analog for restoring pulsatile growth hormone secretion. Documented safety profile in adults with age-related GH decline. Does not suppress endogenous GH production, unlike exogenous GH.
Truthe take: Sermorelin is the reason we use GHRH analogs instead of injecting growth hormone directly. It restores the body's own pulsatile pattern. Safer, more physiologic, less regulatory risk.
Walker RF — Expert Opinion on Investigational Drugs
Spotlight on tesamorelin in HIV-associated lipodystrophy
Tesamorelin (Egrifta™) is a synthetic analog of human growth hormone-releasing hormone (also known as growth hormone-releasing factor) that stimulates the synthesis and release of endogenous growth hormone. It is the first and, so far, only...
Dhillon S — BioDrugs : clinical immunotherapeutics, biopharmaceuticals and gene therapy
Identification of CJC-1295, a growth-hormone-releasing peptide, in an unknown pharmaceutical preparation
Several peptide drugs are being manufactured illicitly, and in some cases they are being made available to the public before entering or completing clinical trials. At the request of Norwegian police and customs authorities, unknown pharmaceutical...
Henninge J, Pepaj M, Hullstein I et al. — Drug testing and analysis
Tesamorelin
In November 2010, tesamorelin (Egrifta; Theratechnologies/EMD Serono), a growth hormone-releasing factor analogue, was approved by the US Food and Drug Administration for the reduction of excess abdominal fat in HIV-infected patients with lipodyst...
Grunfeld C, Dritselis A, Kirkpatrick P — Nature reviews. Drug discovery
Activation of the GH/IGF-1 axis by CJC-1295, a long-acting GHRH analog, results in serum protein profile changes in normal adult subjects
To identify biomarkers of growth hormone (GH) and insulin-like growth factor 1 (IGF-1) action in human serum.
Sackmann-Sala L, Ding J, Frohman LA et al. — Growth hormone & IGF research : official journal of the Growth Hormone Research Society and the International IGF Research Society
Efficacy of ipamorelin, a novel ghrelin mimetic, in a rodent model of postoperative ileus
Ghrelin and ghrelin mimetics stimulate appetite and enhance gastric motility. The present study investigates whether ipamorelin, a selective growth hormone secretagogue and agonist of the ghrelin receptor, would accelerate gastrointestinal transit...
Venkova K, Mann W, Nelson R et al. — The Journal of pharmacology and experimental therapeutics
Sermorelin: a review of its use in the diagnosis and treatment of children with idiopathic growth hormone deficiency
Sermorelin, a 29 amino acid analogue of human growth hormone-releasing hormone (GHRH), is the shortest synthetic peptide with full biological activity of GHRH. Intravenous and subcutaneous sermorelin specifically stimulate growth hormone secretion...
Prakash A, Goa KL — BioDrugs : clinical immunotherapeutics, biopharmaceuticals and gene therapy
Pulsatile secretion of growth hormone (GH) persists during continuous stimulation by CJC-1295, a long-acting GH-releasing hormone analog
Pulsatile GH secretion is considered important for many of the hormone's physiological effects. Short-term GHRH infusions enhance GH pulsatility and increase IGF-I, but the short GHRH half-life limits its therapeutic use. A synthetic GHRH analog (...
Ionescu M, Frohman LA — The Journal of clinical endocrinology and metabolism
Once-daily administration of CJC-1295, a long-acting growth hormone-releasing hormone (GHRH) analog, normalizes growth in the GHRH knockout mouse
Although the majority of children with isolated growth hormone (GH) deficiency have a good growth response to GH-releasing hormone (GHRH), the use of this therapeutic agent is limited by its very short half-life. Indeed, we have shown that, in mic...
Alba M, Fintini D, Sagazio A et al. — American journal of physiology. Endocrinology and metabolism
Prolonged stimulation of growth hormone (GH) and insulin-like growth factor I secretion by CJC-1295, a long-acting analog of GH-releasing hormone, in healthy adults
Therapeutic use of GHRH to enhance GH secretion is limited by its short duration of action.
Teichman SL, Neale A, Lawrence B et al. — The Journal of clinical endocrinology and metabolism
Drug evaluation: tesamorelin, a synthetic human growth hormone releasing factor
Theratechnologies, under license from Valeant, is developing tesamorelin as a potential vaccine adjuvant and for the potential treatment of wasting, hip fracture recovery, immune disorders, HIV-related lipodystrophy, sleep maintenance insomnia and...
Tomlinson B — Current opinion in investigational drugs (London, England : 2000)
Human growth hormone-releasing factor (hGRF)1-29-albumin bioconjugates activate the GRF receptor on the anterior pituitary in rats: identification of CJC-1295 as a long-lasting GRF analog
In vivo bioconjugation to the free thiol on Cys34 of serum albumin by a strategically placed reactive group on a bioactive peptide is a useful tool to extend plasma half-life. Three maleimido derivates of human GH-releasing factor (hGRF)(1-29) wer...
Jetté L, Léger R, Thibaudeau K et al. — Endocrinology
Mechanism of ipamorelin-evoked insulin release from the pancreas of normal and diabetic rats
To examine the effect of ipamorelin (IPA), a novel pentapeptide with a strong growth hormone releasing potency, on insulin secretion from pancreatic tissue fragments of normal and diabetic rats.
Adeghate E, Ponery AS — Neuro endocrinology letters
PEGylation of growth hormone-releasing hormone (GRF) analogues
Synthetically produced GRF1-29 (Sermorelin) has an amino acid composition identical to the N-terminal 29 amino acids sequence of the natural hypothalamic GHRH1-44 (Figure 1). It maintains bioactivity in vitro and is almost equally effective in eli...
Esposito P, Barbero L, Caccia P et al. — Advanced drug delivery reviews
Influence of chronic treatment with the growth hormone secretagogue Ipamorelin, in young female rats: somatotroph response in vitro
Growth hormone (GH) is secreted in the anterior pituitary gland by the somatotroph cells. Secretion is regulated by growth hormone releasing hormone (GHRH) and somatostatin. Morever, GH secretagogues (GHS) can exert a considerable effect on GH sec...
Jiménez-Reina L, Cañete R, de la Torre MJ et al. — Histology and histopathology
The growth hormone secretagogue ipamorelin counteracts glucocorticoid-induced decrease in bone formation of adult rats
The ability of the growth hormone secretagogue (GHS) Ipamorelin to counteract the catabolic effects of glucocorticoid (GC) on skeletal muscles and bone was investigated in vivo in an adult rat model. Groups of 8-month-old female rats were injected...
Andersen NB, Malmlöf K, Johansen PB et al. — Growth hormone & IGF research : official journal of the Growth Hormone Research Society and the International IGF Research Society
Pharmacokinetic-pharmacodynamic modeling of ipamorelin, a growth hormone releasing peptide, in human volunteers
To examine the pharmacokinetics (PK) and pharmacodynamics (PD) of ipamorelin, a growth hormone (GH) releasing peptide, in healthy volunteers.
Gobburu JV, Agersø H, Jusko WJ et al. — Pharmaceutical research
Pharmacokinetic evaluation of ipamorelin and other peptidyl growth hormone secretagogues with emphasis on nasal absorption
1. The pharmacokinetics of three new peptidyl growth hormone secretagogues, ipamorelin (NNC 26-0161), NNC 26-0194 and NNC 26-0235, were compared with two well-known hexapeptides, GHRP-2 and GHRP-6, in the male rat following different routes of adm...
Johansen PB, Hansen KT, Andersen JV et al. — Xenobiotica; the fate of foreign compounds in biological systems
A new series of highly potent growth hormone-releasing peptides derived from ipamorelin
A new series of GH secretagogues derived from ipamorelin is described. In an attempt to obtain oral bioavailability, by reducing the size and the number of potential hydrogen-bonding sites of the compounds, a strategy using the peptidomimetic frag...
Ankersen M, Johansen NL, Madsen K et al. — Journal of medicinal chemistry