Drug intelligence / Profile preview

sulfamethoxazole + hydroxyurea + azacytidine + cytarabine + thioguanine

Development stage
Unknown
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

**Sulfamethoxazole + hydroxyurea + azacytidine + cytarabine + thioguanine** is a five-drug combination without a standardized brand name or protocol identifier in clinical use. **Sulfamethoxazole**, a sulfonamide antibiotic, inhibits bacterial folate synthesis by competitively inhibiting dihydropteroate synthase. **Hydroxyurea**, an antimetabolite, inhibits ribonucleotide reductase, disrupting DNA synthesis and elevating fetal hemoglobin in sickle cell disease. **Azacytidine**, a hypomethylating agent (cytidine nucleoside analog), incorporates into RNA and DNA, inhibiting DNA methyltransferases to reactivate silenced genes and induce differentiation/apoptosis in myeloid cells. **Cytarabine**, a pyrimidine analog, inhibits DNA polymerase after activation to cytarabine triphosphate, causing chain termination primarily in S-phase cells. **Thioguanine**, a purine analog, is converted to thioguanine nucleotides that incorporate into DNA/RNA, disrupting nucleic acid synthesis. This combination merges antimicrobial prophylaxis (sulfamethoxazole) with intensive antineoplastic activity targeting DNA metabolism, likely for high-risk hematologic malignancies like acute myeloid leukemia (AML) in immunosuppressed patients, though no specific trial or approval exists for this exact regimen.

02

Targets

DNA polymerase familyRNR (Ribonucleotide reductase)CYP2C9 (Cytochrome P450 family 2 subfamily C member 9)DNMT1 (DNA (cytosine-5)-methyltransferase 1)DHPS (Dihydropteroate synthase)DNA

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