isavuconazonium
Trade name: cresemba
Small moleculeapprovedOrphan Drug FDA
Approved
Mar 6, 2015
Isavuconazole is an active form of isavuconazonium, a prodrug which is marketed under the name Cresemba. Isavuconazole inhibits lanosterol 14-alpha demethylase (or CYP51A1) and leads to the accumulation of ergosterol toxic precursors in the fungal cytoplasm. Isavuconazole is indicated for the treatment of invasive aspergillosis and invasive mucormycosis. — NCATS
Clinical trial activity
42 trials · 16 clinical orgs · 1 marketing orgs
Phase 1
27
Phase 2
12
Phase 3
7
Phase 4
1
Earliest trial started May 1, 2006 (NCT00413439)
Timeline
Indications
Studied for
- Aspergillosis · Phase 3
- Candidemia · Phase 3
- Candidiasis, Invasive · Phase 3
- Healthy Volunteers · Phase 1
- Hematologic Neoplasms · Phase 2
- Immunocompromised Host · Phase 3
- Invasive Fungal Infections · Phase 3
- Invasive Pulmonary Aspergillosis · Phase 2
- Kidney Diseases · Phase 1
- Leukemia, Myeloid, Acute · Phase 2/Phase 3
- Lung Diseases · Phase 3
- Lymphoma · Phase 2
- Mycoses · Phase 4
- Myelodysplastic Syndromes · Phase 2
- Myeloproliferative Disorders · Phase 2
- Neutropenia · Phase 2
- Pharmacokinetics · Phase 1
- Pharmacological and Toxicological Phenomena · Phase 1
- SARS-CoV-2 · Phase 3
Mechanism of action
- Lanosterol 14-alpha demethylaseINHIBITOR
Lanosterol 14-alpha demethylase inhibitor
- Lanosterol 14-alpha demethylaseINHIBITOR
Lanosterol 14-alpha demethylase inhibitor
Approval history
- approvedPriority reviewMar 6, 2015
Chemistry & pharmacology
Loading structure…
SMILES
CNCC(=O)OCc1cccnc1N(C)C(=O)OC(C)[n+]1cnn(C[C@](O)(c2cc(F)ccc2F)[C@@H](C)c2nc(-c3ccc(C#N)cc3)cs2)c1- Mol. weight
- 717.78 g/mol
- Lipinski Ro5
- 2 violation(s)
- Rule of 3
- No
- Chirality
- Racemic Mixture
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral, Parenteral
- Availability
- Prescription Only
Oral
Yes
Parenteral
Yes
Topical
No
Prodrug
Sources
- ChEMBLCHEMBL1183349 ↗
- WikipediaIsavuconazonium ↗
- NCATS60UTO373KE ↗
- ChEMBLCHEMBL409153 ↗
- ChEMBLCHEMBL3137333 ↗
Also known as
- bal8557
- bal 8557
- bal-8557
- bal8557-000
- bal8557-000
- bal8557-000
- bal8557-002
- bal8557-002
- bal8557-002
- cresemba
- cresemba
- cresemba
- cresemba
- cresemba
- isavuconazole
- isavuconazole
- isavuconazole
- isavuconazole
- isavuconazole
- isavuconazonium
- isavuconazonium
- isavuconazonium
- isavuconazonium
- isavuconazonium
- isavuconazonium
- isavuconazonium
- isavuconazonium chloride
- isavuconazonium sulfate
- isavuconazonium sulfate
- isavuconazonium sulfate
- isavuconazonium sulfate
- isavuconazonium sulfate
- isavuconazonium sulfate
- prodrug isavuconazonium sulfate
- ro0098557
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT06440915 | N/A | Jul 1, 2024 | Jiao Tong University |
| NCT05630976 | Phase 4 | Jan 30, 2023 | Pfizer |
| NCT04707703 | Phase 3 | Mar 16, 2021 | Astellas, University of California, Davis, University of California, San Diego |
| NCT04680884 | Phase 3 | Dec 21, 2020 | Assistance Publique - Hôpitaux de Paris |
| NCT04548648 | Phase 2 | Sep 30, 2020 | AstraZeneca, University of North Carolina at Chapel Hill |
| NCT05140096 | Phase 1 | Jan 3, 2020 | Acerta Pharma |
| NCT04096157 | Phase 1 | Sep 30, 2019 | Astellas |
| NCT03964090 | Phase 2 | Jun 26, 2019 | National Cancer Institute (NCI) |
| NCT03816176 | Phase 2 | Mar 18, 2019 | Astellas |
| NCT03471988 | Phase 3 | Apr 16, 2018 | Asahi Kasei Pharma |
| NCT03327727 | Phase 2 | Feb 20, 2018 | Vical |
| NCT03241550 | Phase 1 | Oct 2, 2017 | Astellas, Basilea Pharmaceutica |
| NCT03149055 | Phase 2 | May 4, 2017 | Astellas, Cornell University |
| NCT03019939 | Phase 2 | Mar 28, 2017 | University of Texas at Houston |
| NCT02128321 | Phase 1 | Jan 1, 2014 | Astellas, Basilea Pharmaceutica |
| NCT02128893 | Phase 1 | Jan 1, 2014 | Astellas, Basilea Pharmaceutica |
| NCT01884636 | Phase 1 | Feb 1, 2013 | Astellas, Basilea Pharmaceutica |
| NCT01884558 | Phase 1 | Feb 1, 2013 | Astellas, Basilea Pharmaceutica |
| NCT01813461 | Phase 1 | Oct 1, 2012 | Astellas, Basilea Pharmaceutica |
| NCT01635946 | Phase 1 | Aug 1, 2012 | Astellas, Basilea Pharmaceutica |
Showing 20 of 42 trials
Page 1 / 3
Organizations
Research & Development (16)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Astellas | For profit | 32 | 30 | 3 | 2006 |
| Basilea Pharmaceutica | For profit | 29 | 1 | 2 | 2006 |
| Acerta Pharma | For profit | 1 | 1 | 1 | 2020 |
| Asahi Kasei Pharma | For profit | 1 | 1 | 1 | 2018 |
| Assistance Publique - Hôpitaux de Paris | Academic/Hospital | 1 | 1 | 1 | 2020 |
| AstraZeneca | For profit | 1 | 0 | 1 | 2020 |
| Cornell University | Academic/Hospital | 1 | 1 | 1 | 2017 |
| Jiao Tong University | Academic/Hospital | 1 | 1 | 1 | 2024 |
| National Cancer Institute (NCI) | Government | 1 | 1 | 1 | 2019 |
| Pfizer | For profit | 1 | 1 | 1 | 2023 |
| University of California, Davis | Academic/Hospital | 1 | 0 | 1 | 2021 |
| University of California, San Diego | Academic/Hospital | 1 | 1 | 1 | 2021 |
| University of Cologne | Academic/Hospital | 1 | 0 | 1 | 2006 |
| University of North Carolina at Chapel Hill | Academic/Hospital | 1 | 1 | 1 | 2020 |
| University of Texas at Houston | Academic/Hospital | 1 | 1 | 1 | 2017 |
| Vical | For profit | 1 | 1 | 1 | 2018 |
16 organizations
Page 1 / 1
Marketing (1)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Astellas | For profit | NDA | Mar 6, 2015 |