Carrier based drug delivery system
AssigneeCyclacel Limited
InventorsPeter M. Fischer, Shudong Wang, Nikolai Zhelev
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Abstract
The present invention relates to a novel drug delivery system of use in the improved delivery of drug therapeutic agents into target cells. The system comprises a drug moiety linked to a carrier moiety wherein the carrier moiety comprises a homeobox peptide or a fragment or derivative thereof.
Claims40
A macromolecule comprising a drug moiety linked to a carrier moiety, wherein the carrier moiety is a fragment of a homeobox peptide or a derivative of the fragment consisting of between 7 and 15 amino acids, wherein the drug moiety is a therapeutically active non-peptide, non-oligonucleotide, non-cholesterol, non-biotin containing drug, and the carrier moiety facilitates the cellular internalization of the drug moiety.
A macromolecule comprising a drug moiety, a linker moiety, and a carrier moiety selected from the group consisting of the combination of drug moiety, linker moiety and carrier moiety set forth on each line below:
- Drug moiety Linker moiety Carrier moiety (methotrexate)4 ((methylamino)benzoyl-EGβA)4 (L)3βARQIKIWFQNRRMKWKK-OH doxorubicin succinimidobenzoyl-C RQIKIWFQNRRMKWKK-OH doxorubicin succinimidobenzoyl-C (D-K)(D-K)(D-W)(D-K)(D-M)(D- R)(D-R)(D-N)(D-Q)(D-F)(D-W)(D- I)(D-K)(D-I)(D-Q)(D-R-NH2) paclitaxel 2′-succinimidopropionoyl-C RQIKIWFQNRRMKWKK-OH N-term- 2′-succinimidopropionoyl-GCG RQIKIWFQNRRMKWKK paclitaxel βA C-term- carboxyfluorescein paclitaxel 2′-succinimidopropionoyl-C RQIKIWFQNRRMKWKK-NH2 paclitaxel 2′-succinimidopropionoyl-CβA RRMKWKK-NH2 paclitaxel 7-succinimidopropionoyl-C RQIKIWFQNRRMKWKK-OH podophyllotoxin 4-succinimidopropionoyl-C RQIKIWFQNRRMKWKK-OH N-term- 4-succinimidopropionoyl-GCG RQIKIWFQNRRMKWKK podophyllotoxin βA C-term- biotinamidocaproyl podophyllotoxin 4-succinimidopropionoyl-C RQIKIWFQNRRMKWKK-NH2 podophyllotoxin 4-succinimidopropionoyl-C (D-R)(D-Q)(D-I)(D-K)(D-I)(D-W)(D- F)(D-Q)(D-N)(D-R)(D-R)(D-M)(D- K)(D-W)(D-K)(D-K-NH2) podophyllotoxin 4-succinimidopropionoyl-CβA RRMKWKK-NH2 podophyllotoxin 4-succinimidopropionoyl-CβA (D-R)(D-R)(D-M)(D-K)(D-W)(D- K)(D-K-NH2) epipodophyllotoxin 4′-succinimidopropionoyl-C RQIKIWFQNRRMKWKK-OH epipodophyllotoxin 4′-succinimidopropionoyl-C RQIKIWFQNRRMKWKK-NH2 epipodophyllotoxin 4′-succinimidopropionoyl-CβA RRMKWKK-NH2 4′-demethyl 4-succinimidopropionoyl-C RQIKIWFQNRRMKWKK-OH epipodophyllotoxin etoposide (G2, G3 and succinimidopropionoyl-C RQIKIWFQNRRMKWKK-OH 4′) roscovotine succinimidopropionoyl-C RQIKIWFQNRRMKWKK-OH bohemine βA-succinyl-βA RQIKIWFQNRRMKWKK-OH bohemine succinimidopropionoyl-C RQIKIWFQNRRMKWKK-OH podophyllotoxin 4-acetyl-C RQIKIWFQNRRMKWKK-OH podophyllotoxin 4-acetyl-CβA RRMKWKK-NH2 4′-demethyl 4-acetyl-CβA RRMKWKK-NH2 epipodophyllotoxin 4′-demethyl 4-acetyl-C RQIKIWFQNRRMKWKK-NH2 epipodophyllotoxin podophyllotoxin 4-succinimidopropionoyl-GCβA RRMKWKK-NH2 camptothecin 10-O-succinimidopropionoyl-C RQIKIWFQNRRMKWKK-NH2 N-term- 4-succinimidopropionoyl-C RRMKWKK podophyllotoxin 4-succinimidopropionoyl-C C-term- podophyllotoxin N-term- 4′-succinimidopropionoyl-C RRMKWKK epipodophyllotoxin 10-O-succinimidopropionoyl-C C-term- camptothecin N-term- 4′-succinimidopropionoyl-C RRMKWKK epipodophyllotoxin 2′-(succinimido)propionoyl-C C-term paclitaxel 4′-methoxy- 4-(4″-aminoanilino) RQIKIWFQNRRMKWKK-NH2 epipodophyllotoxin succinimidopropionoyl-C 4′-methoxy- 4-(4″-aminoanilino) RRMKWKK-NH2 epipodophyllotoxin succinimidopropionoyl-CβA 4′-demethyl- 4-(4″-aminoanilino) RRMKWKK-NH2 epipodophyllotoxin succinimidopropionoyl-CβA (L)3βARQIKIWFQNRRMKWKK corresponds with SEQ ID No.16;
- RQIKIWFQNRRMKWKK corresponds with SEQ ID No. 25;
- and RRMKWKK corresponds with SEQ ID No. 26.
Dependencies are inferred from the claim text.