- 2600 BC – Egyptian physician Imhotep recommended producing a localised infection to promote regression of tumours. According to the Ebers medical papyrus, this was done by placing a poultice near the tumour, followed by local incision.
- BC – Ancient Greeks, Romans, and Egyptians used heat to treat masses. Healers in ancient India used regional and whole-body hyperthermia as treatments.
- 2 AD – Ancient Greeks describe surgical treatment of cancer.
- 1820s – British Dr. James Arnott, "the father of modern cryosurgery", starts to use cryotherapy to freeze tumours in the treatment of breast and uterine cancers
- 1866 – French Dr. Victor Despeignes, "the father of radiation therapy", starts to use X-rays to treat cancer
- 1880s – American Dr. William Stewart Halsted develops radical mastectomy for breast cancer
- 1890s – German Dr. Westermark used localized hyperthermia to produce tumour regression in patients
- 1891 – American Dr. William B. Coley, "the father of immunotherapy", starts to treat cancer patients by injecting them with streptococci, containing immunostimulatory CpG motifs
- 1896 – American Dr. Emil Grubbe starts to treat breast cancer patients with X-rays
- 1900 – Swedish Dr. Stenbeck cures a skin cancer with small doses of radiation
- 1920s – Dr. William B. Coley's immunotherapy treatment, regressed tumors in hundreds of cases, the success of Coley's Toxins attracted heavy resistance from his rival and supervisor, Dr. James Ewing, who was a fanatical supporter of radiation therapy for cancer. This rivalry and opposition to Dr. Coley leads to the disuse of immunotherapy for cancer, in favor of Dr. Ewing's preferred radiation therapy
- 1939 – American Dr. Charles Huggins uses synthetic hormone therapy to treat prostate cancer
- 1942 – First chemotherapy drug mustine used to treat cancer
- 1947 – American Dr. Sidney Farber induces brief remission in a patient with leukaemia with the antifolate drug aminopterin (methotrexate)
- 1949 – US FDA approves mechlorethamine, a nitrogen mustard compound, for treatment of cancer
- 1949 – Oncolytic viruses began human clinical trials
- 1951 – Dr. Jane C. Wright demonstrated the use of the antifolate, methotrexate in solid tumors, showing remission in breast cancer
- 1950s – Anti-cancer anthracyclines isolated from the Streptomyces peucetius bacteria. Anthracycline-based derivatives include: daunorubicin, doxorubicin, amrubicin, idarubicin
- 1953 – US FDA approves Mercaptopurine (6 MP), an immunosuppressive agent
- 1956 – Metastatic choriocarcinoma cancer is cured with the antifolate, methotrexate
- 1957 – Introduction of fluorouracil to treat colorectal, breast, stomach, and pancreatic cancers
- 1957 – Introduction of interferon to treat kidney, skin, and bladder cancer
- 1958 – Combination therapy consisting of 6-mercaptopurine and methotrexate results in a cure of leukaemia in a trial run in US hospitals
- 1958 – US FDA approves cyclophosphamide for chemotherapy of cancer
- 1960s – Introduction of laser therapy in treatment of cancer
- 1960 – Invention of tamoxifen breast cancer anti-estrogen (SERM) hormonal therapy drug
- 1961 – Vincristine, anti-cancer alkaloid, isolated from the Madagascar periwinkle plant
- 1962 – US FDA disapproves Dr. Coley's immunotherapy, making it illegal; radiation therapy remained the dominant treatment for cancer
- 1963 – US FDA approves vincristine (Oncovin) for chemotherapy of cancer
- 1964 – VAMP regimen combination therapy, consisting of: vincristine, amethopterin, 6-mercaptopurine, and prednisone, induces long-term remissions in juvenile acute lymphoblastic leukemia
- 1965 – MOPP regimen combination therapy cures advanced Hodgkin's lymphoma, with the combination of: nitrogen mustard, vincristine, procarbazine, and prednisone
- 1965 – MOMP regimen combination therapy, consisting of: methotrexate, vincristine, 6-MP, and prednisone, induces long-term remissions in juvenile acute lymphoblastic leukemia
- 1965 – Latvian scientist Aina Muceniece identifies echovirus as a potential agent for oncolytic virotherapy, resulting in the development of RIGVIR
- 1966 – Taxol, anti-cancer compound, isolated from the yew plant
- 1967 – Camptothecin, anti-cancer compound, isolated from the Camptotheca acuminata, the Chinese Happy Tree, which was used as a cancer treatment in traditional Chinese medicine. It is the source of chemotherapy drugs: topotecan and irinotecan.
- 1968 – Japanese Dr. Tanaka pioneers the treatment of metastatic breast cancer with cryoablation, resulting in prolonged survival
- 1972 – UK and other European countries approve tamoxifen for breast cancer
- 1972 – American Dr. Lawrence Einhorn cures metastatic testicular cancer with cisplatin
- 1975 – Invention of monoclonal antibodies
- 1975 – American Dr. Einhorn shows combination therapy consisting of cisplatinum, vinblastine, and bleomycin can cure 70% of advanced testicular cancer cases
- 1975 – C-MOPP regimen combination therapy, consisting of: methotrexate, vincristine, cyclophosphamide, and prednisone, cured advanced diffuse large B-cell lymphoma
- 1977 – US FDA approves tamoxifen for metastatic breast cancer only, not widely popular as chemotherapy remains first line of treatment
- 1981 – American Dr. Bernard Fisher proves lumpectomy is as effective as mastectomy for breast cancer
- 1989 – US FDA approves Carboplatin, a derivative of cisplatin, for chemotherapy
- 1990 – US FDA approves tamoxifen for major additional use to help prevent the recurrence of cancer in "node-negative" patients
- 1990 – China begins treating various cancers with photodynamic therapy
- 1991 – First gene therapy treatment of cancer (melanoma)
- 1992 – Invention of tyrosine-kinase inhibitor Imatinib
- 1992 – Invention of Etacstil breast cancer anti-estrogen (SERM/SERD) hormonal therapy drug that overcomes hormone-therapy resistance
- 1996 – US FDA approves antiestrogen, aromatase inhibitor Anastrozole for advanced breast cancer
- 1996 – Russia begins treating various cancers with photodynamic therapy
- 1997 – First monoclonal antibody, Rituximab, is licensed
- 1997 – Chinese doctors start treating uterine fibroids, liver cancer, breast cancer, pancreatic cancer, bone tumours, and renal cancer with ultrasound imaging-guided High-intensity focused ultrasound
- 1998 – Chinese doctors start treating breast, kidney, lung, liver, prostate and bone cancer with imaging-guided cryoablation
- 1998 – US FDA approves herceptin, a monoclonal antibody for HER2 metastatic breast cancer
- 1998 – US FDA approves cryoablation for the treatment of prostate cancer
- 1998 – US FDA approves Camptothecin-analogue irinotecan for chemotherapy of cancer
- 1998 – US FDA approves tamoxifen to reduce breast cancer risk in high-risk patients
- 1998 – US FDA approves monoclonal antibody, Trastuzumab for advanced HER-2 breast cancer
- 1998 – Imaging-guided High-intensity focused ultrasound is approved for use in Europe for treatment of cancer
- 2001 – UK NICE approves taxol for chemotherapy of breast, ovarian, and non-small cell lung cancers
- 2002 – US FDA approves imatinib
- 2002 – Chinese FDA approves Gendicine, gene therapy for cancer
- 2002 – Corporate takeover of Dupont by BMS resulted in abandoning Etacstil breast cancer anti-estrogen (SERM/SERD) hormonal therapy drug that overcomes hormone-therapy resistance
- 2003 – American Dr. Peter Littrup starts to treat early and metastatic breast cancer with cryoablation
- 2004 – bevacizumab, the first approved drug to inhibit blood vessel formation by tumours, is licensed
- 2005 – US FDA approves taxol for chemotherapy of breast, pancreatic, and non-small cell lung cancers
- 2006 – US FDA approves herceptin
- 2007 – US FDA approves sorafenib
- 2007 – US FDA approves camptothecin-analogue topotecan for chemotherapy of cancer
- 2010 – US FDA approves immunotherapy, sipuleucel-T dendritic cell vaccine for advanced prostate cancer
- 2010 – China advances cryoimmunotherapy to treat breast, kidney, lung, liver, prostate and bone cancer
- 2011 – US FDA approves monoclonal antibody, Ipilimumab for advanced melanoma
- 2011 – Cuba develops and releases CimaVax-EGF, the first therapeutic cancer vaccine for lung cancer
- 2012 – Cuba develops and releases monoclonal antibody, Racotumomab, the therapeutic cancer vaccine for lung cancer
- 2015 – US FDA approves anti-CDK4/6, Palbociclib for advanced breast cancer
- 2015 – US FDA approves imaging-guided High-intensity focused ultrasound for prostate cancer