Evidence Grade C — Moderate human evidence. 377 published studies, 250 human. 0 registered clinical trials.
Medically reviewed by a licensed medical professional
This entry covers abaloparatide's use in male osteoporosis. The same drug is approved as Tymlos for postmenopausal osteoporosis in women (see the separate abaloparatide entry). Male osteoporosis is an underserved area where fewer treatment options have been formally studied and approved compared to female osteoporosis.
Abaloparatide (Male Osteoporosis) is also known by these brand and alternate names:
377 published studies: 250 human, 40 animal, 17 in-vitro, 149 reviews
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.
Abaloparatide activates the PTH1 receptor with a preference for the receptor conformation that produces bone-building (anabolic) effects over the conformation associated with bone breakdown. This results in net bone formation. The mechanism is the same as described under compound #29 — the investigation is whether the efficacy demonstrated in postmenopausal women translates to men with osteoporosis.
Abaloparatide received FDA approval for male osteoporosis in December 2022, based on a trial of 228 men showing significant bone density improvements. The fracture reduction evidence comes from the larger ACTIVE trial in women (2,463 patients), which demonstrated an 86% reduction in vertebral fractures. The preclinical bone tumour warning limits treatment to a maximum of two years, though post-marketing surveillance has not confirmed this risk in humans. Sequential therapy with an anti-resorptive agent after stopping abaloparatide is recommended to maintain bone density gains. The failed transdermal patch development means injection remains the only delivery option. See the main abaloparatide entry for full clinical details.
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Abaloparatide (brand name Tymlos in the US, Eladynos in the EU) is a 34-amino-acid PTHrP(1-34) analog peptide developed by Radius Health/Ipsen. Molecular weight approximately 3,960 Da. CAS number: 247062-33-5. Administered as 80 microgram daily subcutaneous injection. IMPORTANT CORRECTION: the male osteoporosis indication was FDA-approved on December 20, 2022, making this an approved rather than purely investigational entry. Original postmenopausal osteoporosis approval was April 2017. EU approval was granted December 2022.
Abaloparatide selectively agonizes the PTH1 receptor with preferential binding to the RG (G-protein coupled) receptor conformation rather than the R0 conformation preferred by teriparatide. This produces more transient cAMP signaling, resulting in a greater net anabolic bone-forming effect with lower calcium-mobilizing potential and reduced risk of hypercalcemia compared with teriparatide. The selective receptor conformation binding differentiates the molecular pharmacology from both PTH(1-34) and PTH(1-84).
The ACTIVE pivotal trial (NCT01343004; N=2,463 postmenopausal women) demonstrated 86% relative risk reduction in new vertebral fractures versus placebo (P<0.0001), with lumbar spine BMD increase of +11.2% versus +0.6% placebo. ACTIVExtend (N=1,139) showed 43-month combined treatment with sequential abaloparatide followed by alendronate produced 84% vertebral fracture risk reduction. The ATOM trial (NCT03512262; N=228 men with osteoporosis) demonstrated lumbar spine BMD increase of +8.5% versus +1.2% placebo (P<0.0001), with total hip and femoral neck BMD also significantly improved, supporting the male osteoporosis approval. The wearABLe transdermal patch delivery trial did not meet non-inferiority criteria versus subcutaneous injection.
The information on this page is provided for educational and research reference purposes only. This is not medical advice. Always consult a qualified healthcare professional before making any health-related decisions.
Linaclotide is marketed as Linzess (approved August 2012). It is taken as a daily oral capsule on an empty stomach, at least 30 minutes before the first meal. The recommended dose is 290 mcg for IBS-C and 72 or 145 mcg for chronic constipation. In clinical trials, approximately 34% of IBS-C patients met the composite improvement endpoint compared to 17% on placebo. Diarrhoea is the most common side effect (approximately 20%) and the leading reason for discontinuation. Linaclotide has a boxed warning against use in children under 6 years due to deaths in young mice, though no such events have been reported in humans. It competes with plecanatide (which targets the same pathway) and other IBS-C treatments.
Elamipretide (Forzinity) was approved by the FDA for Barth syndrome based on the TAZPOWER trial. The randomised crossover phase (12 patients) did not meet its primary endpoints, but the open-label extension (168 weeks) demonstrated durable improvements in walking distance and muscle strength that formed the basis for approval. Barth syndrome affects approximately 1 in 300,000–400,000 births. A larger Phase III trial in primary mitochondrial myopathy (218 patients, MMPOWER-3) did not meet its primary endpoint, and the drug was not approved for that broader indication. Elamipretide remains approved exclusively for Barth syndrome. See also SS-31 (#158) for the research compound context.
Glucagon has been available as an emergency injection since the 1960s and remains the standard rescue treatment for severe hypoglycaemia. Recent innovation has focused on making it easier to administer in emergencies. Baqsimi, approved in 2019, was the first needle-free option as a nasal powder. Gvoke, also approved in 2019, eliminated the need to mix and reconstitute the medication before injection — a significant advance since severe hypoglycaemia often impairs the ability to follow complex preparation steps. Dasiglucagon (Zegalogue), a next-generation stable liquid glucagon approved in 2021, further improved on the convenience of rescue administration. Beyond emergency rescue, glucagon's receptor is now a major research target — dual and triple agonists combining glucagon receptor activity with GLP-1 (such as survodutide and retatrutide) are in advanced clinical trials for obesity and metabolic disease.
This content is for informational purposes only and does not constitute medical advice. Always consult a qualified healthcare professional before making decisions about your health.
