# An Overview of Anticoagulant Drugs Pharmacology, Therapeutic Approaches, Limitations and Perspectives

**Authors:** Claudiu Morgovan, Adina Frum, Laurentiu Stoicescu, Anca Butuca, Carmen Maximiliana Dobrea, Anca Maria Arseniu, Adriana Aurelia Chis, Maria Lucia Muresan, Felicia Gabriela Gligor, Ioana Rada Popa Ilie, Steliana Ghibu

PMC · DOI: 10.3390/pharmaceutics18020163 · 2026-01-26

## TL;DR

This paper reviews anticoagulant drugs, their uses, limitations, and recent advancements in treating conditions like venous thrombosis.

## Contribution

The paper provides a comprehensive overview of new anticoagulant drugs and their therapeutic benefits compared to older treatments.

## Key findings

- New oral anticoagulants like dabigatran and rivaroxaban improve patient adherence and reduce bleeding risks.
- Reversal agents for new anticoagulants have been developed for emergency situations.
- Alternative anticoagulants for heparin-induced thrombocytopenia include argatroban and lepirudin.

## Abstract

Coagulation is a physiological process necessary to achieve homeostasis. Many pathologies lead to spontaneous activation of the coagulation pathways and increase the risk of venous thrombosis (e.g., atrial fibrillation, orthopaedic surgery, cancer). Therefore, a lot of patients need anticoagulant drugs as preventive or curative treatment. In general, older molecules (unfractionated heparin, low-molecular-weight heparins, vitamin K antagonists) have good efficacy. Still, their adverse reactions, increased risk of bleeding, or difficult administration led to low adherence to treatment and had even limited their use. Recently, new molecules were authorised to improve patient adherence to treatment, mainly formulated for oral administration (e.g., dabigatran, rivaroxaban, apixaban, etc.). This therapeutic approach has a low risk of bleeding and does not require special monitoring by laboratory tests. Also, new anticoagulants for patients with heparin-induced thrombocytopenia (e.g., argatroban, lepirudin, bivalirudin, etc.) were obtained. Moreover, reversal agents for the new anticoagulant molecules used in overdoses or in situations where immediate cessation of the anticoagulant effect is required (e.g., emergency surgery) were studied, some of them being authorised on the pharmaceutical market. This narrative review aims to provide a pharmacological and therapeutic overview of anticoagulant drugs, underlining their implementation and limitations.

## Linked entities

- **Chemicals:** dabigatran (PubChem CID 216210), rivaroxaban (PubChem CID 6433119), apixaban (PubChem CID 10182969), argatroban (PubChem CID 92722), lepirudin (PubChem CID 118856773), bivalirudin (PubChem CID 16129704)
- **Diseases:** atrial fibrillation (MONDO:0004981), heparin-induced thrombocytopenia (MONDO:0018048)

## Full-text entities

- **Genes:** CYP2C9 (cytochrome P450 family 2 subfamily C member 9) [NCBI Gene 1559] {aka CPC9, CYP2C, CYP2C10, CYPIIC9, P450-2C9, P450IIC9}, SERPINC1 (serpin family C member 1) [NCBI Gene 540261] {aka AT3}, CYP3A4 (cytochrome P450 family 3 subfamily A member 4) [NCBI Gene 1576] {aka CP33, CP34, CYP3A, CYP3A3, CYPIIIA3, CYPIIIA4}, F2 (coagulation factor II, thrombin) [NCBI Gene 2147] {aka PT, RPRGL2, THPH1}, GGCX (gamma-glutamyl carboxylase) [NCBI Gene 2677] {aka VKCFD1, VKGC}, BGLAP (bone gamma-carboxyglutamate protein) [NCBI Gene 632] {aka BGP, OC, OCN}, F10 (coagulation factor X) [NCBI Gene 2159] {aka FX, FXA}, ABCB1 (ATP binding cassette subfamily B member 1) [NCBI Gene 5243] {aka ABC20, CD243, CLCS, ENPAT, GP170, MDR1}, APOB (apolipoprotein B) [NCBI Gene 338] {aka FCHL2, FLDB, LDLCQ4, apoB-100, apoB-48}, F11 (coagulation factor XI) [NCBI Gene 2160] {aka FXI, PTA}, FN1 (fibronectin 1) [NCBI Gene 2335] {aka CIG, ED-B, FINC, FN, FNZ, GFND}, IL6 (interleukin 6) [NCBI Gene 3569] {aka BSF-2, BSF2, CDF, HGF, HSF, IFN-beta-2}, CYP3A5 (cytochrome P450 family 3 subfamily A member 5) [NCBI Gene 1577] {aka CP35, CYPIIIA5, P450PCN3, PCN3}, CRP (C-reactive protein) [NCBI Gene 1401] {aka PTX1}, F3 (coagulation factor III, tissue factor) [NCBI Gene 2152] {aka CD142, TF, TFA}, FGF2 (fibroblast growth factor 2) [NCBI Gene 2247] {aka BFGF, FGF-2, FGFB, HBGF-2}, SERPINC1 (serpin family C member 1) [NCBI Gene 462] {aka AT3, AT3D, ATIII, ATIII-R2, ATIII-T1, ATIII-T2}, KLK4 (kallikrein related peptidase 4) [NCBI Gene 9622] {aka AI2A1, ARM1, EMSP, EMSP1, KLK-L1, PRSS17}, CYP1A2 (cytochrome P450 family 1 subfamily A member 2) [NCBI Gene 1544] {aka CP12, CYPIA2, P3-450, P450(PA)}, CXCL8 (C-X-C motif chemokine ligand 8) [NCBI Gene 3576] {aka GCP-1, GCP1, IL8, LECT, LUCT, LYNAP}, PROC (protein C, inactivator of coagulation factors Va and VIIIa) [NCBI Gene 5624] {aka APC, PC, PROC1, THPH3, THPH4}, NFKB1 (nuclear factor kappa B subunit 1) [NCBI Gene 4790] {aka CVID12, EBP-1, KBF1, NF-kB, NF-kB1, NF-kappa-B1}, F5 (coagulation factor V) [NCBI Gene 2153] {aka FVL, PCCF, RPRGL1, THPH2, fV}, VWF (von Willebrand factor) [NCBI Gene 7450] {aka F8VWF, VWD}, F7 (coagulation factor VII) [NCBI Gene 2155] {aka SPCA}, LRP1 (LDL receptor related protein 1) [NCBI Gene 4035] {aka A2MR, APOER, APR, CD91, DDH3, IGFBP-3R}, F9 (coagulation factor IX) [NCBI Gene 2158] {aka F9 p22, FIX, HEMB, P19, PTC, THPH8}, ANPEP (alanyl aminopeptidase, membrane) [NCBI Gene 290] {aka AP-M, AP-N, APN, CD13, GP150, LAP1}, VEGFA (vascular endothelial growth factor A) [NCBI Gene 7422] {aka L-VEGF, MVCD1, VEGF, VPF}, F13A1 (coagulation factor XIII A chain) [NCBI Gene 2162] {aka F13A}, HRG (histidine rich glycoprotein) [NCBI Gene 3273] {aka HPRG, HRGP, THPH11}, FGB (fibrinogen beta chain) [NCBI Gene 2244] {aka HEL-S-78p}, CYP4F3 (cytochrome P450 family 4 subfamily F member 3) [NCBI Gene 4051] {aka CPF3, CYP4F, CYPIVF3, LTB4H}, PF4 (platelet factor 4) [NCBI Gene 5196] {aka CXCL4, PF-4, SCYB4}, PPIG (peptidylprolyl isomerase G) [NCBI Gene 9360] {aka CARS-Cyp, CYP, SCAF10, SRCyp}, PLG (plasminogen) [NCBI Gene 5340] {aka HAE4}, TNF (tumor necrosis factor) [NCBI Gene 7124] {aka DIF, IMD127, TNF-alpha, TNFA, TNFSF2, TNLG1F}, APOH (apolipoprotein H) [NCBI Gene 350] {aka B2G1, B2GP1, BG}, CES1 (carboxylesterase 1) [NCBI Gene 1066] {aka ACAT, CE-1, CEH, CES2, HMSE, HMSE1}, IL1B (interleukin 1 beta) [NCBI Gene 3553] {aka IL-1, IL1-BETA, IL1F2, IL1beta}, CYP2C19 (cytochrome P450 family 2 subfamily C member 19) [NCBI Gene 1557] {aka CPCJ, CYP2C, CYPIIC17, CYPIIC19, P450C2C, P450IIC19}, F12 (coagulation factor XII) [NCBI Gene 2161] {aka HAE3, HAEX, HAF}
- **Diseases:** peripheral arterial embolism (MESH:D058729), embolic events (MESH:D004617), rhinitis (MESH:D012220), DDIs (MESH:D000081015), ischemic attack (MESH:D002546), congestive heart failure (MESH:D006333), spinal injury (MESH:D013124), breast cancer (MESH:D001943), Renal Impairment (MESH:D007674), postoperative infections (MESH:D013530), thromboembolic (MESH:D013923), hepatic toxicity (MESH:D056486), contact hypersensitivity (MESH:D003877), Liver Failure (MESH:D017093), heart disease (MESH:D006331), Hypersensitivity (MESH:D004342), ovarian cancer (MESH:D010051), MNPT (MESH:D007020), dyspepsia (MESH:D004415), necrosis (MESH:D009336), Gastrointestinal and intracranial haemorrhages (MESH:D006471), disseminated intravascular coagulation (MESH:D004211), unstable angina (MESH:D000789), aphthous stomatitis (MESH:D013281), overdose (MESH:D062787), sepsis (MESH:D018805), haemophilia (MESH:D006467), lupus anticoagulant (MESH:C531622), lichen planus (MESH:D008010), microvascular disorders (MESH:D017566), transient (MESH:C563551), Thrombotic (MESH:D013927), portal and mesenteric vein thrombosis (MESH:D012170), metastases (MESH:D009362), hypertension (MESH:D006973), occlusion of (MESH:D001157), death (MESH:D003643), VTE (MESH:D054556), hip fracture (MESH:D006620), viral infection (MESH:D014777), intracranial bleeding (MESH:D013345), haemorrhagic stroke (MESH:D002543), ATIII deficiency (MESH:D020152), atherosclerosis (MESH:D050197), myocardial infarction (MESH:D009203), oedema (MESH:C536897), infections (MESH:D007239), type III and type IV hypersensitivity (MESH:D006968), Coagulation (MESH:D001778), Cardiovascular diseases (MESH:D002318), gastrointestinal diseases (MESH:D005767), Thrombocytopenia (MESH:D013921), AF (MESH:D001281), COVID-19 (MESH:D000086382), HIT (MESH:C562865), ischemic complications (MESH:D017202), post-thrombotic syndrome (MESH:D000094025), ischemic stroke (MESH:D002544), endothelial injury (MESH:D057772), Cerebrovascular Diseases (MESH:D002561)
- **Chemicals:** amiodarone (MESH:D000638), idrabiotaparinux (MESH:C545956), ardeparin (MESH:C093450), griseofulvin (MESH:D006118), ATP (MESH:D000255), ximelagatran (MESH:C426686), fluconazole (MESH:D015725), cephalin (MESH:D010714), itraconazole (MESH:D017964), Rivaroxaban (MESH:D000069552), glycol (MESH:D006018), cysteine (MESH:D003545), melagatran (MESH:C109573), carbamazepine (MESH:D002220), digoxin (MESH:D004077), reviparin (MESH:C094240), dermatan sulfate (MESH:D003871), S-warfarin (MESH:D014859), ellagic acid (MESH:D004610), verapamil (MESH:D014700), certoparin (MESH:C403769), hydrogen (MESH:D006859), Heparin (MESH:D006493), 3,3'-methylene-bis-(4-hydroxycoumarin (MESH:D001728), semuloparin (MESH:C569346), gamma-carboxyglutamic acid (MESH:D015055), Bemiparin (MESH:C411345), LMWH (MESH:D006495), barbiturates (MESH:D001463), calcium (MESH:D002118), vitamin K 2,3-epoxide (MESH:C016186), acenocoumarol (MESH:D000074), folic acid (MESH:D005492), ARC2172 (-), celite (MESH:D007692), cisplatin (MESH:D002945), clopidogrel (MESH:D000077144), Heparan sulfates (MESH:D006497), phenylbutazone (MESH:D010653), sulfamethoxazole (MESH:D013420), hydroxychloroquine (MESH:D006886), Doxorubicin (MESH:D004317), silica (MESH:D012822), glycosaminoglycan (MESH:D006025), idraparinux (MESH:C479958), oligosaccharide (MESH:D009844), nadroparin (MESH:D017762), Charcoal (MESH:D002606), D-glucuronic acid (MESH:D020723), Betrixaban (MESH:C543086), cholestyramine (MESH:D002792), nitroglycerin (MESH:D005996), Vitamin K (MESH:D014812), dexamethasone (MESH:D003907), Heparinoids (MESH:D006496), cephalosporins (MESH:D002511), phenytoin (MESH:D010672), Dabigatran (MESH:D000069604), fluvoxamine (MESH:D016666), lenalidomide (MESH:D000077269)
- **Species:** Glycyrrhiza glabra (species) [taxon 49827], Selaginella bryopteris (species) [taxon 1229519], Hypericum perforatum (species) [taxon 65561], Bos taurus (bovine, species) [taxon 9913], Mentha x piperita (peppermint, species) [taxon 34256], Uncaria tomentosa (species) [taxon 128375], Hydrastis canadensis (goldenseal, species) [taxon 13569], Valeriana officinalis (common valerian, species) [taxon 19953], Prunus avium (gean, species) [taxon 42229], Rattus norvegicus (brown rat, species) [taxon 10116], Citrus x aurantium (bitter orange, species) [taxon 43166], Hirudo medicinalis (medicinal leech, species) [taxon 6421], Vipera berus berus (common viper, subspecies) [taxon 31156], Heterometrus laoticus (species) [taxon 217256], Homo sapiens (human, species) [taxon 9606], Citrus bergamia (bergamot orange, species) [taxon 380129], Eucalyptus globulus (blue gum, species) [taxon 34317], Silybum marianum (blessed milkthistle, species) [taxon 92921], Allium sativum (garlic, species) [taxon 4682], Citrus x paradisi (grapefruit, species) [taxon 37656]
- **Mutations:** Ile-Trp, V66M
- **Cell lines:** MDA-MB-231 — Homo sapiens (Human), Breast adenocarcinoma, Cancer cell line (CVCL_0062), HaCaT — Homo sapiens (Human), Spontaneously immortalized cell line (CVCL_0038), NCI-H460 lung cancer — Homo sapiens (Human), Lung large cell carcinoma, Cancer cell line (CVCL_0459)

## Figures

7 figures with captions in the complete paper: https://tomesphere.com/paper/PMC12943893/full.md

---
Source: https://tomesphere.com/paper/PMC12943893