Overview
Doxorubicin is a cytotoxic anthracycline antibiotic isolated from cultures of Streptomyces peucetius var. caesius along side with daunorubicin, another cytotoxic agent, in 1970. Although they both have aglyconic and sugar moieties, doxorubicin's side chain terminates with a primary alcohol group compared to the methyl group of daunorubicin. Although its detailed molecular mechanisms have yet to be understood, doxorubicin is generally thought to exert its effect through DNA intercalation, which eventually leads to DNA damage and the generation of reactive oxygen species. Thanks to its efficacy and broad effect, doxorubicin was approved by the FDA in 1974 to treat a variety of cancer, including but not limited to breast, lung, gastric, ovarian, thyroid, non-Hodgkin’s and Hodgkin’s lymphoma, multiple myeloma, sarcoma, and pediatric cancers. However, one of the major side effects of doxorubicin is cardiotoxicity, which excludes patients with poor heart function and requires treatment termination once the maximally tolerated cumulative dose is reached.
Indication
Doxorubicin is indicated for the treatment of neoplastic conditions like acute lymphoblastic leukemia, acute myeloblastic leukemia, Hodgkin and non-Hodgkin lymphoma, metastatic breast cancer, metastatic Wilms’ tumor, metastatic neuroblastoma, metastatic soft tissue and bone sarcomas, metastatic ovarian carcinoma, metastatic transitional cell bladder carcinoma, metastatic thyroid carcinoma, metastatic gastric carcinoma, and metastatic bronchogenic carcinoma. Doxorubicin is also indicated for use as a component of adjuvant therapy in women with evidence of axillary lymph node involvement following resection of primary breast cancer. For the liposomal formulation, doxorubicin is indicated for the treatment of ovarian cancer that has progressed or recurred after platinum-based chemotherapy, AIDS-Related Kaposi's Sarcoma after the failure of prior systemic chemotherapy or intolerance to such therapy, and multiple myeloma in combination with bortezomib in patients who have not previously received bortezomib and have received at least one prior therapy.
Associated Conditions
- AIDS-related Kaposi's Sarcoma
- Acute Lymphoblastic Leukemia (ALL)
- Acute Myeloid Leukemia
- Advanced Endometrial Cancer
- Advanced Ovarian Cancer
- Breast Cancer
- Hodgkin's Lymphoma
- Metastatic Bone Sarcomas
- Metastatic Breast Cancer
- Metastatic Soft Tissue Sarcoma
- Metastatic Thyroid Cancer
- Metastatic Urothelial Cancer
- Multiple Myeloma (MM)
- Mycosis Fungoides (MF)
- Non-Hodgkin's Lymphoma (NHL)
- Sezary Syndrome
- Waldenström's Macroglobulinemia (WM)
- Advanced Thymoma
- Advanced uterine sarcoma
- Metastatic Bronchogenic Carcinoma
- Metastatic Gastric carcinoma
- Metastatic Neuroblastoma
- Metastatic Ovarian carcinoma
- Metastatic Wilms' tumor
Research Report
A Comprehensive Monograph on Doxorubicin: Chemistry, Pharmacology, and Clinical Application
Part I: Foundational Characteristics
Section 1: Introduction and Drug Identification
1.1. Overview and Historical Context
Doxorubicin is a cytotoxic anthracycline antibiotic that has served as a cornerstone of cancer chemotherapy for over half a century.[1] Its broad spectrum of activity against both hematologic malignancies and solid tumors has cemented its role in numerous first-line and salvage treatment regimens. The drug's development is a landmark in the history of oncology, representing a pivotal moment in the discovery of potent antineoplastic agents from natural sources. It is recognized as such a critical medication that it is included on the World Health Organization's List of Essential Medicines.[1]
The story of doxorubicin begins in the 1950s with a concerted effort by Farmitalia Research Laboratories in Italy to discover anticancer compounds from soil-dwelling microorganisms.[4] This search led to the isolation of a novel strain of
Streptomyces peucetius from a soil sample collected near the 13th-century Castel del Monte in Apulia, Italy.[4] This bacterium produced a vibrant red pigment, an antibiotic that demonstrated significant activity against tumors in murine models. Concurrently, researchers at Rhône-Poulenc in France isolated the same compound, which they named Rubidomycin due to its ruby color.[6] The two teams ultimately combined their nomenclature to create the generic name
daunorubicin, a portmanteau of "Dauni," a pre-Roman tribe from the Italian region of discovery, and "rubis," the French word for ruby.[5] Clinical trials in the 1960s confirmed daunorubicin's efficacy in treating acute leukemia and lymphoma, but by 1967, its potential to induce fatal cardiac toxicity became a significant clinical concern.[4]
Clinical Trials
Title | Posted | Study ID | Phase | Status | Sponsor |
---|---|---|---|---|---|
2025/07/22 | Not Applicable | Not yet recruiting | |||
2025/07/22 | Not Applicable | Not yet recruiting | |||
2025/07/18 | Not Applicable | Not yet recruiting | |||
2025/07/11 | Not Applicable | Recruiting | |||
2025/07/03 | Not Applicable | Not yet recruiting | |||
2025/06/30 | Not Applicable | Not yet recruiting | |||
2025/06/25 | Phase 1 | Not yet recruiting | |||
2025/06/24 | Phase 2 | Not yet recruiting | |||
2025/06/15 | Phase 2 | Not yet recruiting | Michael Spinner, MD | ||
2025/06/11 | Phase 2 | Not yet recruiting | Vandana Abramson |
FDA Drug Approvals
Approved Product | Manufacturer | NDC Code | Route | Strength | Effective Date |
---|---|---|---|---|---|
Baxter Healthcare Company | 0338-0080 | INTRAVENOUS | 2 mg in 1 mL | 5/31/2022 | |
Baxter Healthcare Corporation | 0338-0080 | INTRAVENOUS | 2 mg in 1 mL | 5/31/2022 | |
Hikma Pharmaceuticals USA Inc. | 0143-9089 | INTRAVENOUS | 2 mg in 1 mL | 1/16/2024 | |
Gland Pharma Limited | 68083-248 | INTRAVENOUS | 2 mg in 1 mL | 5/15/2023 | |
NorthStar RxLLC | 72603-103 | INTRAVENOUS | 2 mg in 1 mL | 7/12/2022 | |
Hikma Pharmaceuticals USA Inc. | 0143-9085 | INTRAVENOUS | 2 mg in 1 mL | 1/16/2024 | |
Athenex Pharmaceutical Division, LLC. | 70860-208 | INTRAVENOUS | 2 mg in 1 mL | 10/20/2017 | |
BluePoint Laboratories | 68001-345 | INTRAVENOUS | 2 mg in 1 mL | 9/28/2022 | |
Hikma Pharmaceuticals USA Inc. | 0143-9087 | INTRAVENOUS | 2 mg in 1 mL | 1/16/2024 | |
NorthStar RxLLC | 72603-200 | INTRAVENOUS | 2 mg in 1 mL | 7/12/2022 |
EMA Drug Approvals
Approved Product | Authorization Holder | Status | Issued Date |
---|---|---|---|
Authorised | 9/15/2022 | ||
Authorised | 7/13/2000 | ||
Authorised | 6/20/1996 |
HSA Drug Approvals
Approved Product | Manufacturer | Approval Number | Dosage Form | Strength | Approval Date |
---|---|---|---|---|---|
DOXORUBICIN ADVAGEN CONCENTRATE FOR SOLUTION FOR INFUSION 2MG/ML | SIN16420P | INJECTION, SOLUTION, CONCENTRATE | 2.0 mg/ml | 1/25/2022 | |
ADRIM – DOXORUBICIN HYDROCHLORIDE INJECTION USP 2MG/ML | SIN16081P | INJECTION, SOLUTION | 2 mg/ml | 1/15/2021 | |
CAELYX CONCENTRATE FOR INFUSION 2 mg/ml | SIN10426P | INJECTION | 2.00 mg/ml | 11/16/1998 | |
DOXORUBICIN-TEVA CONCENTRATE FOR SOLUTION FOR INFUSION 2 MG/ML | SIN14969P | INJECTION, SOLUTION, CONCENTRATE | 2mg/ml | 3/21/2016 | |
DOXOCCORD CONCENTRATE FOR SOLUTION FOR INFUSION 2 MG/ML | SIN16284P | INFUSION, SOLUTION CONCENTRATE | 2 mg/ml | 7/23/2021 | |
K. U. DOXORUBICIN HCL FOR INJECTION 10 mg/vial | SIN10992P | INJECTION, POWDER, FOR SOLUTION | 10 mg/vial | 6/26/1999 | |
K. U. DOXORUBICIN HCL FOR INJECTION 50 mg/vial | SIN10991P | INJECTION, POWDER, FOR SOLUTION | 50 mg/vial | 6/26/1999 | |
CHEMODOX CONCENTRATE FOR INFUSION 2MG/ML | SIN16102P | INJECTION, SOLUTION | 2MG/ML | 2/9/2021 | |
ADRIAMYCIN CS INJECTION 2 mg/ml | SIN10566P | INJECTION | 2 mg/ml | 12/18/1998 | |
DOXABIN INJECTION 2MG/ML | Mylan Laboratories Limited [OTL] | SIN14262P | INJECTION, SOLUTION | 2mg/ml | 10/30/2012 |
NMPA Drug Approvals
Approved Product | Company | Approval Number | Drug Type | Dosage Form | Approval Date |
---|---|---|---|---|---|
No NMPA approvals found for this drug. |
PPB Drug Approvals
Approved Product | Registration No. | Company | Licence No. | Strength | Registration Date |
---|---|---|---|---|---|
No PPB approvals found for this drug. |
TGA Drug Approvals
Approved Product | ARTG ID | Sponsor | Registration Type | Status | Registration Date |
---|---|---|---|---|---|
Doxorubicin hydrochloride injection 50 mg in 25 mL (18) | 332664 | Medicine | A | 3/27/2020 | |
Doxorubicin hydrochloride Injection 200 mg in 100 mL (7) | 317063 | Medicine | A | 5/1/2019 | |
Doxorubicin hydrochloride injection 10 mg in 5 mL (14) | 313876 | Medicine | A | 2/1/2019 | |
Doxorubicin hydrochloride injection 10 mg in 5 mL (8) | 307723 | Medicine | A | 8/2/2018 | |
Doxorubicin Injection 10 mg/5 mL (21) | 406166 | Medicine | A | 3/14/2023 | |
LIPOSOMAL DOXORUBICIN SUN Doxorubicin Hydrochloride 20mg/10mL Liposome Injection concentrate glass vial | 202826 | Medicine | A | 12/11/2013 | |
Doxorubicin Hydrochloride Injection 50 mg/25 mL (1) | 285782 | Medicine | A | 2/16/2017 | |
Doxorubicin hydrochloride injection 20 mg in 10 mL (3) | 308160 | Medicine | A | 8/13/2018 | |
Doxorubicin hydrochloride injection 50 mg in 25 mL (15) | 310294 | Medicine | A | 10/11/2018 | |
Doxorubicin hydrochloride injection 10 mg in 5 mL (13) | 313875 | Medicine | A | 2/1/2019 |
Health Canada Drug Approvals
Approved Product | Company | DIN | Dosage Form | Strength | Market Date |
---|---|---|---|---|---|
ADRIAMYCIN RDF | 02069563 | Powder For Solution - Intravenous | 150 MG / VIAL | 12/31/1996 | |
DOXORUBICIN HCL FOR INJ. U.S.P. 150MG/VIAL | david bull laboratories (pty) ltd. | 02093081 | Powder For Solution - Intravenous | 150 MG / VIAL | 12/31/1995 |
DOXORUBICIN HYDROCHLORIDE FOR INJECTION USP | 02194465 | Powder For Solution - Intravesical
,
Intravenous | 50 MG / VIAL | 7/30/1997 | |
PEGYLATED LIPOSOMAL DOXORUBICIN HYDROCHLORIDE FOR INJECTION | dr reddy's laboratories ltd | 02544857 | Suspension - Intravenous | 2 MG / ML | N/A |
ADRIAMYCIN RDF INJ 50MG/VIAL | carlo erba farmitalia spa | 00353078 | Powder For Solution - Intravenous | 50 MG / VIAL | 12/31/1976 |
CAELYX | baxter corporation | 02238389 | Suspension - Intravenous | 2 MG / ML | 8/19/1998 |
DOXORUBICIN HYDROCHLORIDE INJECTION | teva canada limited | 02409275 | Solution - Intravenous
,
Intravesical | 2 MG / ML | 2/27/2014 |
DOXORUBICIN INJECTION, BP | 02381982 | Solution - Intravenous
,
Intravesical | 2 MG / ML | 12/16/2014 | |
ADRIAMYCIN PFS | 02071002 | Solution - Intravenous
,
Intravesical | 2 MG / ML | 12/31/1995 | |
DOXORUBICIN HYDROCHLORIDE FOR INJECTION USP | panda pharmaceuticals inc. | 02467240 | Powder For Solution - Intravenous | 50 MG / VIAL | N/A |
CIMA AEMPS Drug Approvals
Approved Product | Company | Registration Number | Pharmaceutical Form | Prescription Type | Status |
---|---|---|---|---|---|
MYOCET LIPOSOMAL 50 MG POLVO, DISPERSION Y DISOLVENTE PARA CONCENTRADO PARA DISPERSION PARA PERFUSION | 00141001 | POLVO PARA CONCENTRADO PARA DISPERSION PARA PERFUSION | Uso Hospitalario | Commercialized |
Philippines FDA Drug Approvals
Approved Product | Company | License Number | Dosage Form | Strength | Approval Date |
---|---|---|---|---|---|
No Philippines FDA approvals found for this drug. |
Saudi SFDA Drug Approvals
Approved Product | Company | License Number | Dosage Form | Strength | Approval Date |
---|---|---|---|---|---|
No Saudi SFDA approvals found for this drug. |
Malaysia NPRA Drug Approvals
Approved Product | Company | Registration Number | Dosage Form | Strength | Approval Date |
---|---|---|---|---|---|
No Malaysia NPRA approvals found for this drug. |
UK EMC Drug Information
Medicine Name | MA Holder | MA Number | Pharmaceutical Form | Active Ingredient | Authorization Date |
---|---|---|---|---|---|
No UK EMC drug information found for this drug. |
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