Evidence Grade A — Regulatory approved. 1903 published studies. 89 registered clinical trials.
Medically reviewed by a licensed medical professional
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Bivalirudin (sold as Angiomax) is a hospital blood thinner given through an IV drip during heart procedures such as coronary stenting. Originally inspired by the natural anticoagulant found in medicinal leeches, it is especially valuable for patients who cannot safely receive heparin. Its effects wear off predictably within about 25 minutes of stopping the infusion, giving doctors precise control.
Bivalirudin is also known by these brand and alternate names:
1,903 published studies: 1611 human, 25 animal, 60 in-vitro, 503 reviews
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.
Bivalirudin grabs thrombin — the key enzyme that converts fibrinogen into fibrin clots — at two separate points simultaneously, blocking both its active site and its fibrinogen-binding site. This dual grip provides powerful and specific anticoagulation. Crucially, thrombin slowly chews through the bivalirudin molecule itself, breaking free over about 25 minutes. This self-limiting mechanism means anticoagulation wears off predictably and quickly once the infusion stops — a significant safety advantage over heparin, which can be unpredictable and requires monitoring.
Bivalirudin's evidence comes from large cardiology trials involving thousands of patients. The HORIZONS-AMI trial showed a 40% reduction in major bleeding compared to heparin-based regimens in heart attack patients. However, it was also linked to a higher rate of early stent clotting, which tempered initial enthusiasm. The drug's clinical niche has narrowed over time. It was originally positioned as a safer alternative when used alongside powerful anti-platelet infusions, but as those infusions fell out of routine use, the bleeding advantage over heparin alone became less compelling. Today, bivalirudin is used primarily in patients with heparin-induced thrombocytopenia — a dangerous immune reaction to heparin — where a non-heparin anticoagulant is essential. No major new research programmes are active.
PeptideTrace tracks 89 registered clinical trials for Bivalirudin sourced from ClinicalTrials.gov.
Aggrastat Truncated Length Against Standard Therapies in Percutaneous Coronary Intervention
Bivalirudin Versus Heparin During PCI in High Bleeding Risk Patients With Acute Coronary Syndromes
Bivalirudin with Prolonged Infusion During PCI Versus Heparin After Fibrinolytic Therapy
Multicenter Trial of ECMO in Children With Severe Cardiac Failure Using the Cardiohelp System
Use of Bivalirudin for Anticoagulation in Patients With Extracorporeal Membrane Oxygenation
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Bivalirudin is a 20-amino-acid synthetic peptide direct thrombin inhibitor based on the structure of hirudin, the anticoagulant peptide from the medicinal leech (Hirudo medicinalis). It is administered intravenously and has a short half-life of approximately 25 minutes.
Bivalirudin is a bivalent direct thrombin inhibitor: the N-terminal sequence binds thrombin's catalytic active site, while the C-terminal sequence binds exosite-1 (the fibrinogen-binding site). This dual binding provides potent, specific thrombin inhibition. Uniquely, thrombin slowly cleaves bivalirudin at the Arg3-Pro4 bond, making the inhibition reversible and self-limiting. It inhibits both free (circulating) and clot-bound thrombin (unlike heparin, which only inhibits free thrombin). It does not require antithrombin III as a cofactor and carries no risk of HIT.
Bivalirudin is marketed as Angiomax (approved December 15, 2000). Generic available. Indicated for PCI, particularly in patients with or at risk of HIT. HORIZONS-AMI (N=3,602; STEMI PCI): NACE 9.2% versus 12.1% for heparin+GPI (P=0.005); major bleeding 4.9% versus 8.3% (P<0.001); cardiac mortality 1.8% versus 2.9% (P=0.03). However, acute stent thrombosis was higher: 1.3% versus 0.3% (P<0.001). HEAT-PPCI (N=1,812; heparin alone vs bivalirudin alone): heparin was superior when GPIs not used routinely.
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.
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