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Biological Mechanisms of Action of Blockbuster Drugs

Behind every blockbuster drug like Ozempic, Humira, Keytruda, and Eliquis is a specific molecular mechanism. This page breaks down how today's top-prescribed therapies work, from the receptors they bind to the pathways they disrupt, grounded in 138 million peer-reviewed papers from Elicit's citation database.

Browse all mechanisms

A drug's mechanism of action describes how it produces its therapeutic effect at the molecular, cellular, or systemic level. Understanding MOA is essential for drug development, competitive intelligence, and clinical research.

MOA Name

Generic Drug Name

Target

Mechanism

Example Drugs

Indication

AMPK activator, Complex I inhibitor

Dual GIP/GLP-1 receptor agonism→

Tirzepatide

GIPR/GLP1R

Dual GIP and GLP-1 receptor agonist; increases insulin secretion and reduces glucagon levels in a glucose-dependent manner

  • Mounjaro

  • Zepbound

  • Type 2 diabetes mellitus

  • Chronic weight management (obesity or overweight with comorbidities)

  • Obstructive sleep apnea in adults with obesity

Factor Xa inhibition→

Apixaban

F10 (factor X / factor Xa)

Direct, reversible, highly selective inhibitor of factor Xa (FXa); inhibits free and clot-bound FXa to decrease thrombin generation and thrombus development

  • Eliquis

  • Nonvalvular atrial fibrillation (stroke/SE risk reduction)

  • DVT prophylaxis after hip or knee replacement

  • Deep vein thrombosis (DVT) treatment

  • Pulmonary embolism (PE) treatment

  • Recurrent DVT/PE risk reduction

GLP-1 receptor agonism→

Semaglutide

GLP1R

GLP-1 receptor agonist that enhances glucose-dependent insulin secretion; slows gastric emptying; increases pancreatic β-cell proliferation; reduces glucagon release

  • Ozempic

  • Rybelsus

  • Wegovy

  • Type 2 diabetes mellitus (T2DM)

IL-12/IL-23 inhibition→

Ustekinumab

IL12B (p40 subunit shared by IL-12 and IL-23)

Human monoclonal antibody that binds the shared p40 subunit of IL-12 and IL-23, preventing their interaction with the IL-12 receptor β1 subunit and thereby inhibiting IL-12/IL-23–mediated signaling and cytokine production.

  • Stelara

  • Wezlana

  • Imuldosa

  • Otulfi

  • Pyzchiva

  • Selarsdi

  • Steqeyma

  • Yesintek



  • Plaque psoriasis

  • Psoriatic arthritis

  • Crohn's disease

  • Ulcerative colitis




IL-23 inhibition→

Risankizumab

IL23A (IL-23 p19 subunit)

Binds the p19 subunit of IL-23 and inhibits IL-23 from interacting with the IL-23 receptor and subsequent signaling

  • Skyrizi

  • Plaque psoriasis

  • Psoriatic arthritis

  • Crohn's disease

IL-23 inhibition→

Guselkumab

IL-23 (IL23A) / IL-23 receptor (IL23R)

Human IgG1λ monoclonal antibody that binds selectively to IL-23 and inhibits IL-23 bioactivity by blocking IL-23 interaction with the cell-surface IL-23 receptor, disrupting IL-23–mediated signaling, activation, and cytokine cascades

  • Tremfya

  • Plaque psoriasis

  • Psoriatic arthritis

  • Ulcerative colitis

  • Crohn's disease

IL-4/IL-13 pathway inhibition→

Dupilumab

IL4R (IL-4 receptor alpha subunit, IL-4Rα)

Binds IL-4Rα to inhibit IL-4 and IL-13 signaling (dual blockade of type 2 inflammatory pathways)

  • Dupixent

  • Atopic dermatitis

  • Asthma

  • Chronic rhinosinusitis with nasal polyposis

  • Eosinophilic esophagitis

  • Prurigo nodularis

JAK inhibition→

Upadacitinib

JAK1/JAK3

Janus kinase (JAK) inhibitor; in human leukocyte cellular assays, inhibited cytokine-induced STAT phosphorylation mediated by JAK1 and JAK1/JAK3

  • Rinvoq

  • Moderately to severely active ulcerative colitis

  • Moderately to severely active Crohn's disease

Neprilysin inhibition + RAAS blockade→

Sacubitril/Valsartan

Neprilysin (MME) / angiotensin II receptor type 1 (AGTR1)

Neprilysin inhibition plus angiotensin II receptor blockade: sacubitril inhibits neprilysin to prevent breakdown of natriuretic peptides (prolonging favorable effects), while valsartan blocks the RAAS via angiotensin II receptor antagonism

  • Entresto

  • Chronic heart failure in adults

  • Symptomatic heart failure with LV systolic dysfunction (pediatric ≥1 year)

RANKL inhibition→

Denosumab

TNFSF11 (RANKL)

RANK ligand (RANKL) inhibitor that binds RANKL and competitively inhibits its binding to RANK, inhibiting osteoclast formation, function, and survival and reducing bone resorption

  • Prolia

  • Postmenopausal osteoporosis at high fracture risk

  • Osteoporosis in men at high fracture risk

  • Glucocorticoid-induced osteoporosis at high fracture risk

  • Bone loss from androgen deprivation therapy (prostate cancer, men)

  • Bone loss from aromatase inhibitor therapy (breast cancer, women)