Phase I study of intravenous TZT-1027 (T) and carboplatin (C), administered on Day 1 (T and C) and Day 8 (T) every three weeks in patients (pts) with advanced solid tumors

Blagden, Sarah P.; Thomas, Amanda; deBono, Johann S.; Ahmed, Sheikh; Greystoke, Alastair; Attard, Gerhardt; Jenner, A.; Fong, PC; Steward, W.P.

doi:10.1200/jco.2005.23.16_suppl.3141

Cited by 2 publications

(1 citation statement)

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“…In a phase 1 combination study, auristatin PE was administered with carboplatin to patients with solid tumors (82). Auristatin PE (starting dose 0.4 mg/m 2 ) was administered as a 1-h IV on days 1 and 8 q3w, and carboplatin (AUC = 4 or 5) was administered on day 1 as a 30-min IV before auristatin PE, q3w.…”

Section: Auristatin Pe (Tzt-1027 Dolastatin 10 Analog)mentioning

confidence: 99%

Investigational Anticancer Agents Targeting the Microtubule

Vereshchagina¹,

Scharf²,

Colevas

The Role of Microtubules in Cell Biology, Neurobiology, and Oncology

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This chapter summarizes the preclinical and clinical development to date of investigational anticancer agents whose mechanism of action is thought to be via direct interaction with tubulin or microtubules. All of the compounds discussed are agents discovered or derived from screening natural materials for anti-cancer activity. The underlying theme for pursuit of these agents is that tubulin is a validated anticancer target and that novel interactions between new chemical entities and tubulin may overcome resistance, increase therapeutic index, or alter the spectrum of clinical utility against different cancer types.

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Section: Auristatin Pe (Tzt-1027 Dolastatin 10 Analog)mentioning

confidence: 99%

Investigational Anticancer Agents Targeting the Microtubule

Vereshchagina¹,

Scharf²,

Colevas

The Role of Microtubules in Cell Biology, Neurobiology, and Oncology

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A practical approach to asymmetric synthesis of dolastatin 10

Zhou

Nie

et al. 2017

Org. Biomol. Chem.

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Dolastatin 10, an antineoplastic agent for cancer chemotherapy, is a linear peptide possessing N,N-dimethyl Val-OH, l-valine, (3R,4S,5S)-dolaisoleucine, (2R,3R,4S)-dolaproine and (S)-dolaphenine. Our efficient synthesis includes the following three key features: (1) SmI-induced cross-coupling was employed to couple aldehyde 11 with (S)-N-tert-butanesulfinyl imine 12 to generate the required stereocenters of Dap (7); (2) asymmetric addition of chiral N-sulfinyl imine 10 provided a straightforward approach to the synthesis of the protected Doe ((S,S)-8); (3) a practical method to the key subunit Val-Dil (24a) has been established as an alternative synthetic route for the synthesis of this challenging chemical structure.

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Phase I study of intravenous TZT-1027 (T) and carboplatin (C), administered on Day 1 (T and C) and Day 8 (T) every three weeks in patients (pts) with advanced solid tumors

Cited by 2 publications

References 0 publications

Investigational Anticancer Agents Targeting the Microtubule

Investigational Anticancer Agents Targeting the Microtubule

A practical approach to asymmetric synthesis of dolastatin 10

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