Thymidylate synthase inhibitors inhibit the enzyme thymidylate synthase which prevents the methylation of C5 of deoxyuridine monophosphate (dUMP) thereby inhibiting the synthesis of deoxythymidine monophosphate (dTMP). The effect is shown by the promotion of cell death as cells would not be able to properly undergo DNA synthesis if they are lacking dTMP which is a necessary precursor to dTTP. Thymidylate synthase inhibitors are generally indicated for breast cancer, lung cancer, gastric cancer, colorectal cancer, acute lymphocytic leukemia, thoracic cancer, and others. It is also indicated for rheumatoid arthritis and psoriatic arthritis. Roche, Eli Lilly, Taiho Pharmaceutical, Medac Pharma, AstraZeneca, Merck, and Eagle Pharmaceutical are some of the pharmaceutical companies with thymidylate synthase inhibitors in the market. Moreover, some of the companies have thymidylate synthase inhibitors in phase-I/II of clinical trials for cancer indications.
Key Market Developments:
- In Dec 2022, US FDA approved Eagle Pharmaceuticals’ Pemetrexed for non-small cell lung cancer in the USA.
- In Mar 2023, Medac Pharma launched (Metoject) Methotrexate subcutaneous auto-injection for juvenile rheumatoid arthritis, psoriasis, and psoriatic arthritis in Denmark, Portugal, Norway, Germany, Finland, Greece, France, Poland, Spain, Czech Republic, UK, Austria, Netherlands, and Sweden.
- In Apr 2023, Isofol Medical and Oncosyne AS entered into a research collaboration to evaluate the effect of drug candidate Arfolitixorin in different doses combined with the cancer drug 5-FU.
Approved Thymidylate synthase inhibitors:
- LEUCOVORIN (5-Fluorouracil)
- XELODA (Capecitabine)
- ALIMTA (Pemetrexed)
- TEYSUNO (Gimeracil/Oteracil/Tegafur)
- CARAC (Fluorouracil topical)
- TOMUDEX (Raltitrexed)
- FUSILEV (Levoleucovorin calcium)
- FOLOTYN (Pralatrexate)
- UFTORAL (Tegafur/Uracil)
- PEMFEXY (Pemetrexed)
Drugs under the Pipeline for Thymidylate synthase inhibitors:
- Modufolin (Arfolitixorin)
- Orzel (UFT + Leucovorin)
- TG6002
- Fosifloxuridine Nafalbenamide (NUC-3373)
- Furtulon (Doxifluridine)
- LX-101
- CX1106
- TBI 302
- TMV-018
- Thymitaq (Nolatrexed)
- Idetrexed (CT900)
- Irinotecan/Floxuridine (LY01616)
- Vodobatinib (SCO - 088)
Clinical Activity and Developments of Thymidylate synthase inhibitors:
Currently, there are about 10 drug molecules in the market for thymidylate synthase inhibitors with more than 15 drug molecules in clinical trials.
- In Nov 2022, Roche in collaboration with Novartis, Sanofi, Breast International Group, and Agendia completed a phase-III trial for breast cancer in European Union for the drug molecule Capecitabine.
- In Jan 2023, Eli Lilly and Company and Saint John’s Cancer Institute completed a phase-I clinical trial for Chordoma in the USA for IV administration of Pemetrexed.
|
Molecule Name |
Number of Studies |
|
Modufolin (Arfolitixorin) |
7 |
|
Orzel (UFT + Leucovorin) |
4 |
|
TG6002 |
4 |
|
Fosifloxuridine Nafalbenamide (NUC-3373) |
4 |
|
Furtulon (Doxifluridine) |
3 |
|
LX-101 |
2 |
|
CX1106 |
1 |
|
TBI 302 |
1 |
|
TMV-018 |
1 |
|
Thymitaq (Nolatrexed) |
1 |
|
Idetrexed (CT900) |
1 |
|
Irinotecan/Floxuridine (LY01616) |
1 |
Target Indication Analysis of Thymidylate synthase inhibitors
The approved drug molecules like Capecitabine, Methotrexate, Pemetrexed are mainly indicated for cancers such as breast cancer, colorectal cancer, gastric cancer, non-small cell lung cancer, mesothelioma, pancreatic cancer, head and neck cancer, and biliary cancer. These molecules are also used as anti-inflammatories and antipsoriatics in juvenile rheumatoid arthritis, psoriasis, psoriatic arthritis, and rheumatoid arthritis. The drug molecules in clinical trials are being used in conditions such as advanced or metastatic urothelium cancer, pleural biphasic mesothelioma, ovarian cancer, solid tumors, recurrent or metastatic cervical cancer, and others.
Regional Analysis of Thymidylate synthase inhibitors
Thymidylate Synthase Inhibitors Market
According to World Health Organization data 2020, on cancer, China has the highest (8,15,563 new cases) lung cancer incidence rate, followed by the USA (2,27, 875), and for pancreatic cancer also China (1,24,994) was in the top rank, followed by the USA (56,654) and Japan (44,307). Similarly, for bladder cancer, China (85,694 new cases), USA (80,617), and Japan (36,957) are among the top countries. In the case of multiple myeloma USA (32,119 new cases) was at the top. Breast cancer is the most common cancer occurring in women (22,61,419 patients globally), with the highest number of cancer rates in the USA (253,465 patients), followed by France (58,083), and Australia (19,617 patients). Eli Lilly and Company’s Alimta (Pemetrexed) had a total sale of US$ 927 in the year 2022, with US$ 543.7 million sales in the USA only. However, there was a 56% decrease in revenue for Alimta in the USA, primarily driven by decreased demand and new entry of multiple generics in the first half of 2022. Acrotech Pharmaceutical’s Folotyn (Pralatrexate) will see its patent expiration for the treatment of T-cell lymphoma in May 2025.
Latin America
Europe
Asia Pacific
Middle East
North America
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Frequently Asked Questions
LEUCOVORIN (5-Fluorouracil), XELODA (Capecitabine), ALIMTA (Pemetrexed), TEYSUNO (Gimeracil/Oteracil/Tegafur), CARAC (Fluorouracil topical), TOMUDEX (Raltitrexed) are the few approved thymidylate synthase inhibitors.
The total sale of Alimta was US$ US$ 927 in the year 2022.
Roche, Eli Lilly, Taiho Pharmaceutical, Medac Pharma, AstraZeneca, Merck, and Eagle Pharmaceutical are the major players in the thymidylate synthase inhibitors market.
Major indications for thymidylate synthase inhibitors are breast cancer, colorectal cancer, gastric cancer, non-small cell lung cancer, mesothelioma, pancreatic cancer, head and neck cancer, and biliary cancer.
- Novartis AG (Switzerland)
- Eli Lilly and Company (USA)
- Taiho Pharmaceutical (China)
- Medac Pharma (UK)
- Pfizer (USA)
- Gilead Sciences, Inc. (USA)
- Merck (MSD) (USA)
- Roche (Switzerland)
- AstraZeneca (Germany)
- Eagle Pharmaceuticals (USA)