Anidulafungin
JFDA label: Ecalta
Mechanism of Action
Inhibitor of 1,3-beta-glucan synthase — 1,3-beta-glucan synthase inhibitor
| Target | Action | Gene / class |
|---|---|---|
| 1,3-beta-glucan synthase efficacy | INHIBITOR | GSC1 |
Indications
Off-label
- Candidiasis empiric therapy (non-neutropenic ICU patients)
- Candidiasis, chronic disseminated (hepatosplenic)
- Candidiasis, intravascular infections
- Candidiasis, oropharyngeal (refractory disease)
- Candidiasis, osteoarticular infections
Antimicrobial Spectrum
Expected / intrinsic spectrum (EUCAST breakpoints & labels) — not local resistance. Source: openfda-label.
Fungi
| Organism | Activity | MIC |
|---|---|---|
| Candida albicans | Active | — |
| Candida dissemination | Active | — |
| Candida glabrata | Active | — |
| Candida guilliermondii | Active | — |
| Candida krusei | Active | — |
| Candida parapsilosis | Active | — |
| Candida tropicalis | Active | — |
Class profile
| antifungalClass | Echinocandin |
|---|---|
| targetMolecule | Beta-1,3-glucan synthase (FKS1/FKS2 subunit) |
| isFungicidal | 1 |
| spectrumCandida | S (fungicidal) |
| spectrumAspergillus | S (fungistatic) |
| spectrumCryptococcus | Intrinsically resistant |
| spectrumDermatophytes | Resistant |
| resistanceMechanisms | FKS1 hot-spot mutations,FKS2 mutations |
| source | Pappas2016/Lass-Florl2011 |
Contraindications
Source: Lexicomp
- Hypersensitivity to anidulafungin, other echinocandins, or any component of the formulation Absolute
Adverse Reactions
Cardiac disorders (5)
Very Common hypertension · Hypotension · peripheral edema
Common chest pain · Deep vein thrombosis
Nervous system disorders (4)
Very Common Insomnia
Common Confusion · depression · headache
Hepatobiliary disorders (2)
Very Common Increased serum alkaline phosphatase
Common Increased serum transaminases
Renal and urinary disorders (2)
Very Common Urinary tract infection
Common Increased serum creatinine
Blood and lymphatic system disorders (3)
Common Anemia · leukocytosis · thrombocythemia
Metabolism and nutrition disorders (6)
Very Common Hypokalemia · hypomagnesemia
Common dehydration · hyperglycemia · hyperkalemia · Hypoglycemia
Gastrointestinal disorders (7)
Very Common diarrhea · Nausea · vomiting
Common abdominal pain · Constipation · dyspepsia · oral candidiasis
Skin and subcutaneous tissue disorders (1)
Common Decubitus ulcer
Musculoskeletal and connective tissue disorders (1)
Common Back pain
Infections and infestations (2)
Very Common Bacteremia
Common Sepsis
General disorders and administration site conditions (1)
Very Common Fever
Respiratory, thoracic and mediastinal disorders (5)
Very Common Dyspnea
Common cough · Pleural effusion · pneumonia · respiratory distress
Dosing
Source: Lexicomp
Warnings & Precautions
Source: Lexicomp
Anaphylactic reactions
Severe hypersensitivity reactions, including anaphylactic reactions and anaphylactic shock have been reported; immediate treatment for hypersensitivity reactions should be available. Discontinue treatment immediately if reactions occur.
Hepatic effects
Elevated liver function tests, hepatitis, and hepatic failure have been reported; monitor for progressive hepatic impairment if increased transaminase enzymes noted.
Infusion reactions
Infusion reactions (eg, bronchospasm, dyspnea, flushing, hypotension, pruritus, rash, urticaria) may occur; do not exceed recommended rate of infusion. Disease-related concerns:
Candidal infections
Safety and efficacy have not been established in other Candida infections (eg, endocarditis, osteomyelitis, meningitis).
Pregnancy & Lactation
Pregnancy
Adverse effects were observed in animal reproduction studies. Other agents are currently preferred for the treatment of Candida infections in pregnant women (IDSA [Pappas 2016]).
Lactation
It is not known if anidulafungin is present in breast milk. According to the manufacturer, the decision to continue or discontinue breastfeeding during therapy should take into account the risk of infant exposure, the benefits of breastfeeding to the infant, and benefits of treatment to the mother.
Monitoring
| Efficacy | Fungal culture and species identification; minimum inhibitory concentration (MIC) where available; clinical response (temperature, imaging for invasive fungal disease) |
|---|---|
| Toxicity | LFTs (hepatotoxicity — azoles in particular); renal function; ECG for QT prolongation (azoles); drug levels if available (itraconazole, voriconazole) |
| Clinical pearl | Voriconazole levels are highly variable due to CYP2C19 polymorphism — TDM recommended (target trough 2–5 mg/L). Check for drug interactions with CYP3A4 substrates. |
| Counseling | Report visual disturbances (voriconazole), jaundice, or rash. Take azoles with food or as directed to optimise absorption. |
Chemistry & Properties
| Formula | C58H73N7O17 |
|---|---|
| Molecular weight | 1140.25 g/mol |
| IUPAC name | N-[(3S,6S,9S,11R,15S,18S,20R,21R,24S,25S,26S)-6-[(1S,2S)-1,2-dihydroxy-2-(4-hydroxyphenyl)ethyl]-11,20,21,25-tetrahydroxy-3,15-bis[(1R)-1-hydroxyethyl]-26-methyl-2,5,8,14,17,23-hexaoxo-1,4,7,13,16,22-hexazatricyclo[22.3.0.09,13]heptacosan-18-yl]-4-[4-(4-pentoxyphenyl)phenyl]benzamide |
| CAS | 166663-25-8 |
| PubChem CID | 166548 |
| InChIKey | JHVAMHSQVVQIOT-MFAJLEFUSA-N |
SMILES
CCCCCOc1ccc(-c2ccc(-c3ccc(C(=O)N[C@H]4C[C@@H](O)[C@@H](O)NC(=O)[C@@H]5[C@@H](O)[C@@H](C)CN5C(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]([C@H](O)[C@@H](O)c5ccc(O)cc5)NC(=O)[C@@H]5C[C@@H](O)CN5C(=O)[C@H]([C@@H](C)O)NC4=O)cc3)cc2)cc1Biology & Pharmacokinetics
Pharmacokinetics predicted
| Bioavailability | 70.0% |
|---|---|
| Half-life | 3.388 h |
| Volume of distribution | 0.382 L/kg |
| Protein binding | 95.2% |
| BBB penetrant | No |
Enzyme interactions
| Enzyme | Role | Detail |
|---|---|---|
| CYP2B6 | Inhibitor | — |
| CYP2C8 | Inhibitor | IC₅₀ 12.000000000000007 µM |
Transporters
BCRP (Inhibitor)BSEP (Inhibitor)MRP1 (Inhibitor)OATP1B1 (Inhibitor)OATP1B3 (Inhibitor)P-gp (Inhibitor)P-gp (Substrate)
Drug–drug interactions (1, DDInter)
| Interacting drug | Severity | Management |
|---|---|---|
| Cyclosporine | minor |
Registered Products (4)
| Brand | Form / strength | Pack | Agent | Citizen (JOD) |
|---|---|---|---|---|
| Ecalta | Vial 100 mg | 1 vial | Khoury Drug Store | — |
| MUFINES 100 MG LYOPHILIZED POWDER FOR SOLUTION FOR IV INFUSION | Infusion Anidulafungin 100 mg | 1 vial | JAWEDA INT. DRUD STORE | — |
| Nixara | Vial 100 mg | 30 ml | Pharma International Company/ Jordan | — |
| Safdola 100mg/vial powder for concentrate for solution for infusion | Infusion 100 mg | one vial | MS Pharma Jordan | — |