Pluvicto is approved for late-stage prostate cancer (see compound #66). Extended-indication trials are investigating use in earlier disease stages. The PSMAfore trial (468 patients) showed significantly improved progression-free survival in pre-taxane patients. The PSMAddition trial is investigating combination with standard hormonal therapy in metastatic hormone-sensitive prostate cancer. The strategic question is whether moving radioligand therapy earlier in the treatment sequence — when patients have less advanced disease and potentially more PSMA-expressing tumour cells — produces better outcomes. This is not a peptide.

5-Amino-1MQ has no marketing authorisation. No human clinical trials have been conducted. The key preclinical study treated diet-induced obese mice for 11 days and reported body weight and fat mass changes. No human pharmacokinetic, safety, or efficacy data exist. 5-Amino-1MQ is not a peptide. Products available through unregulated channels lack pharmaceutical quality assurance. The absence of any human data means effects, safety, interactions, and appropriate dosing in humans are entirely unknown.

Abaloparatide is marketed as Tymlos (approved April 2017 for postmenopausal osteoporosis; December 2022 for male osteoporosis). In the ACTIVE trial, it reduced vertebral fractures by 86% and non-vertebral fractures by 43% compared to placebo over 18 months. Bone density gains at the hip were numerically greater than with teriparatide. The ACTIVExtend follow-up study showed that patients who transitioned from abaloparatide to the anti-resorptive alendronate maintained their bone gains over an additional two years — the fracture reduction benefit persisted long after the bone-building treatment ended. Like teriparatide, treatment duration is limited to two years. Abaloparatide carries the same preclinical bone tumour warning as teriparatide, though a transdermal patch formulation is in development that could offer a needle-free alternative.

Abaloparatide is approved for postmenopausal osteoporosis (see compound #29). Investigation for male osteoporosis is ongoing. The pivotal ACTIVE trial in women (2,463 patients) demonstrated 86% reduction in vertebral fractures and significant bone density improvements. Male osteoporosis is an underserved population with fewer approved treatment options. See compound #29 for the approved postmenopausal indication and full clinical data.

Abarelix was marketed as Plenaxis (approved November 2003) with a highly restrictive indication — it was only approved for symptomatic advanced prostate cancer where no other treatment options existed, and required a mandatory prescriber registry and monitoring programme. It was withdrawn from the US market in May 2005. The withdrawal was driven by reports of immediate-onset systemic allergic reactions, combined with the restricted indication limiting commercial uptake. Despite its clinical failure, abarelix was historically important as proof that GnRH antagonists could effectively treat prostate cancer without the testosterone flare. This directly enabled the development of degarelix (approved 2008) and relugolix (approved 2020), both of which addressed the safety concerns that ended abarelix's commercial life.

ACE-031 has no marketing authorisation. A Phase I trial in healthy women showed increased lean mass and decreased fat mass. A Phase II trial in DMD (24 patients) showed lean body mass increases but was discontinued due to bleeding-related safety concerns (epistaxis, telangiectasias, and gum bleeding), likely caused by inhibition of BMP-9/10 vascular signalling. ACE-031 is a large fusion protein (~90 kDa), not a peptide. Its clinical development was halted. The non-selective ligand-trapping profile — capturing beneficial vascular signalling molecules alongside the intended muscle-growth targets — illustrates the challenge of targeting the TGF-beta superfamily. Acceleron subsequently developed more selective agents.

Afamelanotide is marketed as Scenesse (Clinuvel Pharmaceuticals, approved October 2019 in the US; previously approved in the EU in 2014). It is delivered as a bioresorbable subcutaneous implant administered every two months. Treatment is only available through a restricted distribution programme. In clinical trials, EPP patients on afamelanotide could spend significantly more time in direct sunlight without pain. EPP is a debilitating condition where even brief light exposure can cause hours of burning pain, and prior to Scenesse there was no approved treatment. Afamelanotide is related to the research compound Melanotan I, but is the only version that has undergone full regulatory approval for a specific medical condition.

Alexamorelin has no marketing authorisation. A Phase II trial (approximately 150 patients) for bowel function recovery after abdominal surgery produced limited results. Published controlled efficacy data are minimal. Ardana Biosciences was acquired by Shire in 2008 and the programme was discontinued. No further clinical development has occurred. The compound is primarily of historical interest within the growth hormone secretagogue research field.

Amycretin is in early-phase development (not yet approved). The oral formulation achieved 13.1% weight loss at just 12 weeks — substantially faster than existing oral options. The subcutaneous formulation achieved 24.3% at 36 weeks. Both results are from Phase I/II trials with relatively small patient numbers. Amycretin's significance lies in its oral formulation achieving weight loss approaching injectable drugs. If the early results are confirmed in larger trials, an effective oral dual-agonist could significantly expand the obesity treatment population. Phase III trials are anticipated.

AOD-9604 has no pharmaceutical authorisation. A Phase IIb obesity trial (536 patients, 12 weeks) of oral AOD-9604 failed to demonstrate significant weight loss compared to placebo. The obesity development programme was discontinued. The developer subsequently pivoted to investigating intra-articular injection for osteoarthritis with preliminary Phase IIa data. The FDA GRAS status (2014) applies exclusively to its use as a food ingredient and does not constitute pharmaceutical approval, authorise therapeutic claims, or establish safety for injectable use. Products available through unregulated channels lack pharmaceutical quality assurance.

ARA-290 (cibinetide) has no marketing authorisation. Phase II trials in sarcoidosis neuropathy showed improvements in corneal nerve fibre density, and a Phase II trial in diabetic neuropathy reported improved metabolic parameters and pain scores. The FDA granted Fast Track designation for sarcoidosis neuropathy. No Phase III trials have been completed. The compound represents an investigational approach to tissue repair that is distinct from existing erythropoietin-based therapies, but its clinical development remains at an early stage.

Argireline has no pharmaceutical authorisation. It is widely available as a cosmetic ingredient in over-the-counter skincare products. Small industry-sponsored studies have reported wrinkle depth reductions of 17–30% with topical application. The key scientific question is whether sufficient peptide penetrates intact skin to reach neuromuscular junctions and produce a meaningful effect. The molecule's size exceeds the conventional limit for transdermal absorption. Argireline's cosmetic use in formulated skincare products represents a fundamentally different risk profile from injectable use.

Bacitracin is marketed as Baciguent (topical) and BACiiM (injection), and is a component of Neosporin and Polysporin. Approved in 1948, it is one of the oldest peptide antibiotics still in widespread use. Topical bacitracin is available over the counter and is applied to minor cuts, scrapes, and burns to prevent infection. Its systemic use is limited to rare situations where no alternatives exist, due to severe nephrotoxicity. There has been growing discussion in wound care about whether routine topical antibiotic use on minor wounds provides meaningful benefit over simple petroleum jelly in keeping wounds moist, and about the risk of contact allergic dermatitis with repeated bacitracin use.

Balixafortide is not approved. The Phase Ib trial (54 evaluable patients) in HER2-negative metastatic breast cancer showed a 30% objective response rate when combined with eribulin chemotherapy. However, the Phase III FORTRESS trial was discontinued after interim futility analysis showed it was unlikely to meet its primary endpoint. Balixafortide's development trajectory illustrates the challenge of translating promising Phase Ib combination therapy results into Phase III confirmation. The compound's clinical development has been discontinued.

Bimagrumab is in Phase II/III development (not yet approved). A Phase II trial (75 patients with type 2 diabetes and obesity) showed 20.5% fat mass reduction with 3.6% lean mass increase — essentially reshaping body composition without net appetite suppression. The BELIEVE Phase IIb trial (507 patients) showed that bimagrumab plus semaglutide achieved 22% weight loss with the weight lost being 88% fat — significantly better body composition than semaglutide alone. Bimagrumab is not a peptide. Its strategic significance is as a combination partner to address the muscle loss problem inherent in weight loss with current obesity drugs. Eli Lilly's acquisition positions it alongside tirzepatide.

Bivalirudin is marketed as Angiomax (approved December 2000), with generic versions available. It is indicated for coronary interventions, particularly in patients with or at risk of heparin-induced thrombocytopenia (HIT) — a dangerous allergic reaction to heparin where the immune system attacks platelets. The HORIZONS-AMI trial in heart attack patients showed bivalirudin reduced major bleeding by 40% compared to heparin plus a GPIIb/IIIa inhibitor. However, it was associated with a higher rate of early stent clotting (acute stent thrombosis), which has tempered enthusiasm. Bivalirudin's role has narrowed as radial artery access (which reduces bleeding) has become standard, but it remains the go-to anticoagulant when heparin cannot be used.

Bortezomib is marketed as Velcade (approved May 2003) for multiple myeloma and mantle cell lymphoma. Generic versions are available. Originally given intravenously, subcutaneous injection is now preferred as it causes significantly less nerve damage. The VISTA trial established bortezomib-based combination therapy as standard for newly diagnosed myeloma patients ineligible for transplant, with median time to disease progression of 24 months versus 16.6 months with older chemotherapy. Peripheral neuropathy (numbness and tingling in hands and feet) is the main dose-limiting side effect, affecting up to 30% of patients. Bortezomib transformed myeloma from a disease with a median survival of approximately 3 years to one where many patients live a decade or more with sequential treatments.

BPC-157 has no marketing authorisation from any major regulatory agency. No human Phase III clinical trials have been completed. The preclinical evidence base consists of over 100 animal studies, predominantly conducted at the University of Zagreb. A small pilot study in ulcerative colitis (4 patients) has been reported but was uncontrolled. No established human dosing, safety profile, or efficacy data from rigorous clinical trials exist. Products available through unregulated channels are not subject to pharmaceutical manufacturing standards, and their composition, purity, and sterility cannot be assured. The gap between the extensive animal literature and the near-complete absence of human clinical data is the defining feature of this compound's evidence base.